avinash dhake - Academia.edu (original) (raw)

Papers by avinash dhake

international journal of chemical sciences, 2009

An estimate of time to reach maximum plasma concentration (tmax) is of paramount importance in as... more An estimate of time to reach maximum plasma concentration (tmax) is of paramount importance in assessing the efficacy of drugs used to treat acute conditions like pain and insomnia, which can be treated by a single dose. This study was conducted to develop Quantitative Structure Pharmacokinetic Relationship (QSPR) for the prediction of tmax in men for congeneric series of 24 quinolone drugs, using computer assisted Hansch approach. The QSPR correlations were duly analyzed using a battery of apt statistical procedures and validated using leave-one-out (LOO) approach. Analysis of several hundreds of QSPR correlations developed in this study revealed high degree of cross-validated coefficients (Q2) using LOO method (p<0.001). The overall predictability was found to be high (R2 = 0.9147 F=33.96 S2=0.0748, Q2=0.8046 p<0.001). Both logarithmic transform and inverse transform of the tmax value resulted in decrease in correlation coefficient (for Log tmax, R2= 0.8636 and for 1/tmax, R2= 0.8701). Topological and electrostatic parameters were found to primarily ascribe the variation in tmax. The results indicate the involvement of dissolution rate limited absorption rather than permeation limited, as hardly any dependence on Log P was observed.

Research Journal of Pharmacy and Technology, Jun 28, 2008

Indian Journal of Pharmaceutical Sciences, 2000

Bioorganic Chemistry, Jul 1, 2022

Thiosemicarbazides (TSCs), dithiocarbamates (DTCs) and their molecular conjugates are promising d... more Thiosemicarbazides (TSCs), dithiocarbamates (DTCs) and their molecular conjugates are promising drug targets. However, hybrids of DTCs with TSCs themselves are rarely investigated. Thus, studies were initiated to synthesize novel system derived from TSC-DTCs to examine their pharmacological applications. The targeted conjugates were designed and synthesized from aryl TSC and aryl DTCs in moderate to good yields. The structures of synthesized compounds were confirmed through FT-IR, 1 H NMR, 13 C NMR and mass spectrometry. The conjugates have been tested for antioxidant and anticancer activities. The in vitro antioxidant activity was performed using 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging assay, hydrogen peroxide scavenging assay and nitric oxide assay and was also compared with aryl DTCs and aryl TSCs to explore potential of newly synthesized hybrids. The preliminary anticancer screening for cytotoxicity was performed using brine shrimp lethality bioassay using Artemia salina shrimps. Anticancer screening was determined against NCI 60 human tumor cell lines at NCI, USA. The results revealed that, newly synthesized hybrids are more active as compared to aryl DTCs and aryl TSCs. Among the tested conjugates for antioxidant screening, 3b was found to be more active than the standard ascorbic acid. The IC 50 value of 3b were 8.96 ± 0.089, 10.7 ± 0.016 and 12.29 ± 0.086 μg/ml for DPPH, hydrogen peroxide scavenging assay and nitric oxide assay respectively, whereas IC 50 values for standard were 11.75 ± 0.015, 12.03 ± 0.107 and 16.66 ± 0.242 μg/ml respectively. Since hybrids are more active than aryl DTCs and aryl TSCs, only newly synthesized hybrids were screened for anticancer potential. For cytotoxicity screening, compound 3b was found to be most active among synthesized conjugates with LD 50 value of 33.86 μg/ ml. For anticancer screening, the compounds 3c and 3d were found to be potent among synthesized series with percent growth inhibition of 22 to 44% when screened against colon cancer cell lines whereas, compound 3b showed growth inhibition of 40% for selective leukemia cell line, K-562. The compounds 3b, 3c and 3d with strong electron-withdrawing groups were found to be the most active antioxidant and anticancer agents among the synthesized conjugates.

Indian Journal of Pharmaceutical Sciences, 2001

A new simple and sensitive spectrophotometric method in the UV region has been developed for the ... more A new simple and sensitive spectrophotometric method in the UV region has been developed for the simultaneous determination of mefenamic acid and paracetamol in bulk and in dosage forms. Mefenamic acid shows three absorbance maxima at 219,284 and 336 nm and paracetamol shows a single absorbance maximum at 257 nm in 0.1N sodium hydroxide. Absorbance corrected for interference was used for estimation. Both these drugs obey Beer's law In the concentration ranges used in this method. The method has been validated statistically and by recovery studies.

Journal of Current Pharma Research, 2013

Currently, inflammatory diseases are being treated with drugs most of which have side effects. Th... more Currently, inflammatory diseases are being treated with drugs most of which have side effects. There is a need to develop newer analogs especially from phytochemical sources that have lesser or no side effects. Hence, we thought it worthwhile to isolate phytosterols from leaves of Tridax procumbens plant, prepare their semisynthetic derivatives and evaluate them for anti-inflammatory activity. Column chromatography and preparative TLC were employed to isolate β-sitosterol and stigmasterol. Their acetylated derivatives were prepared using conventional organic reactions. The compounds were evaluated for invivo anti-inflammatory activity using carrageenan-induced paw oedema method in rats. Results revealed that both β-sitosterol and stigmasterol have significant anti-inflammatory activity viz., 65% and 67%; respectively with standard diclofenac exhibiting 68% inhibition. Derivatives betasitosteryl acetate and stigmasteryl acetate showed 61% and 62% inhibition; respectively. Thus, phytosterols and derivatives of Tridax procumbens leaves can be used as leads to make future drug candidates to treat inflammatory conditions.

Cyclic peptides have emerged as an important class of organic compounds with potent biological ac... more Cyclic peptides have emerged as an important class of organic compounds with potent biological activities like antifungal, antibacterial, anthelmintic, antineoplastic, insecticidal, anti-inflammatory, melanin production inhibitory activities. The inherent medicinal properties of cyclic peptides promoted scientists to isolate these compounds from natural sources. Since only minute quantities are obtained from natural sources, attempts have been made for the synthesis of these compounds in laboratories and biological screening of these compounds gave good results. Number of modifications has been done in the structure of basic cyclic peptides in order to increase their biological activities. Thus there is wide scope for synthesis of these peptides and their derivatives to explore more potent biodynamic molecules. The present review encompasses the idea about the various peptide molecules and their derivatives which have been synthesized in the laboratory and had shown potent biologica...

Green methods such as microwave technique and grinding technique have been found superior over th... more Green methods such as microwave technique and grinding technique have been found superior over the conventional method in view of reaction time and energy requirement. Pyrazoline derivatives , 2a-i and 3a-i, were synthesized both conventional heating and by microwave irradiation, the synthesized compounds were characterized by 1H NMR, 13C NMR, IR and mass spectral analyses. They were screened for their in vitro anti-inflammatory, antimicrobial and antioxidant activities. Antimicrobial activity was performed by Agar plate method and 2d & 2e were active against Gram negative bacteria E. coli and S. aureus, 3c and 3g showed antioxidant activity (IC50=48.13 and 46.03μg/ml),3c shows respectively anti-inflammatory activity at (EC50= 11.00±1.26 µg/mL) 3c ,3d and 3e showed good anti-inflammatory activity at concentration (EC50= 11.70±0.98 µg/mL) & 11.70±0.98 µg/mL respectively.

Green methods such as microwave technique and grinding technique has been found superior over the... more Green methods such as microwave technique and grinding technique has been found superior over the conventional method in view of reaction time and energy requirement. Comp research (2a-i), (3a-i) have been characterized by 1H NMR, 13C NMR, IR and mass spectral analyses. They were screened for their in vitro anti-inflammatory, antimicrobial and in vitro antioxidant activities. Antimicrobial activity was performed by Agar plate method and comp. 2d & 2e a active against gram negative bacteria E. coli and S. aureus, the comp. 3c and 3g show antioxidant activity as (IC50 = 48.13 and 46.03µg/ml), Comp’ 3c shows respectively anti-inflammatory activity at (EC50 = 11.00 ± 1.26 µg/mL). Comp. ,3c ,3d and 3e showed good anti-inflammatory activity at concentration (EC50 = 11.70 ± 0.98 µg/mL) & 11.70 ± 0.98 µg/mL respectively.

Ammannia baccifera Linn, (family Lythraceae), traditionally it is used as cooling appetizer, rubi... more Ammannia baccifera Linn, (family Lythraceae), traditionally it is used as cooling appetizer, rubifacient, laxative, stomachic, diuretic, aphrodisiac and lithotriptic also reported as posses antityphoid and antitubercular.The present study was investigated to evaluate in vitro antimicrobial activity of aqueous, methanolic, hexane extracts against bacteria Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus and against the fungi Candida albicans,Kluyuviromyces mamlamus.The pathogens were tested by disc diffusion assay method, and An attempt has been made to compare the activity of extracts with standard antibiotics against selected pathogen and all the extracts exhibited significant activity.

Bioorganic & Medicinal Chemistry, 2005

In view of obtaining some potential antibacterial compounds, we have described synthesis of some ... more In view of obtaining some potential antibacterial compounds, we have described synthesis of some chloroaryloxyalkyl imidazole and benzimidazole derivatives. The relevant step in the synthetic sequence was the initial condensation of 4-chloro or 2,4-dichlorophenol with 1, n-dibromoalkanes (n=2, 4, 5) to provide compounds 3a-f in sufficient yields. The subsequent condensation of 3a-f with some imidazole derivatives and benzimidazole afforded products 4a-l and 5a-e in good yields. Some of compounds 4a-l as well as 5a-e were tested in vitro against Salmonella typhi O-901 and Staphylococcus aureus A 15091. Compounds 4a and 4c showed considerable bactericidal activities against tested bacteria. Compound 4b showed significant activity against S. aureus A 15091 but was inactive against S. typhi O-901. Other compounds showed intermediate activities against S. aureus A 15091 but most of them were inactive against S. typhi O-901. Semiempirical AM1 calculations showed that negative electrostatic potentials around oxygen of the phenoxy and nitrogen of the imidazole moieties have direct effect on the antibacterial activity towards S. aureus A 15091. In QSAR analysis, different electronic, topologic, functional groups and physicochemical descriptors were calculated for each molecule and a three parametric equation was found between the logMIC and HOMO energy, hydration energy and number of primary carbon atoms of the molecules.

Indian Journal of Pharmaceutical Sciences, 2011

The aim of this study was to evaluate the binding efficiency of mucilage extracted from Dioscorea... more The aim of this study was to evaluate the binding efficiency of mucilage extracted from Dioscorea alata(water yam). The sustained release matrix tablet of Isoniazid was prepared by wet granulation technique using Dioscorea alata Linn. polysaccharide. The polysaccharide was extracted from the tuber via maceration method and evaluated for their color, viscosity and pH.The prepared tablet was evaluated for their hardness, friability, drug content,swelling studies and In vitro dissolution rate. Optimized Formulation F2 and F3 was exhibited satisfactory results as 95 % and 91 % in 12 hrs.whereas formulation F-5 shows 85 % of drug release in 12 hrs. The drug release from the tablet was sustained and non-Fickian transport of drug from the tablet was confirmed. Using Higuchi's Model and the Korsmeyer equation, the drug release mechanism from the sustained release tablets was found to be Anomalous (non-Fickian) diffusion. Compatibility study confirmed that interactions do not exist between the drug and polymer.

Indian Journal of Pharmaceutical Sciences, 2005

A rapid, selective and precise HPLC method for quantification of ofloxacin in tablets has been de... more A rapid, selective and precise HPLC method for quantification of ofloxacin in tablets has been developed. The chromatographic resolution of ofloxacin was achieved using acetonitrile:0.1%v/v triethylamine (20:80, pH-4.0) as the mobile phase, in an isocratic run on a chromatographic system (Waters) equipped with Waters 600 pump controller, 2487 dual I» absorbance detector, Waters32 millennium chromatography manager software and C8 kromasil 5I¼ (4.6x150 mm) column. The flow rate was 1 ml/min and ofloxacin was monitored spectrophotometrically at 280 nm. Ornidazole was used as an internal standard.

RESEARCH AND EDUCATION IN INDIAN …, 2011

Bauhinia variegata Linn (BV), commonly known as Raktkanchan is a medium sized deciduous tree foun... more Bauhinia variegata Linn (BV), commonly known as Raktkanchan is a medium sized deciduous tree found throughout India and traditionally used to cure variety of ailments. In Ayurveda, the plant is documented to be useful as rasayana. The present investigation was planned to evaluate immunomodulatory potential of aqueous (BVA) and ethanol (BVE) extracts of stem bark of BV on neutrophil phagocytic function. The various concentrations (25, 50 and 100 mg/ml) of both the extracts were subjected to study their effects on different in vitro methods of Phagocytosis such as neutrophil locomotion and chemotaxis, immunostimulant activity by Phagocytosis of killed Candida albicans and qualitative nitro blue tetrazolium test using human neutrophils. The results of this preliminary study shown that both the extracts of BV possess stimulatory effect on chemotactic, phagocytic and intracellular killing potency of human neutrophils at the concentration range of 25-100 mg/ml. However, significant activity was revealed by BVE at highest concentration of 100 mg/ml in all the parameters studied. These results suggest that stem bark extracts of B.variegata possess immunomodulatory activity and justifies its use in Ayurveda as rasayana.

Indian Journal of Pharmaceutical Education and Research, 2019

Objective: The objective of present research work is to study in vitro metabolism of risperidone ... more Objective: The objective of present research work is to study in vitro metabolism of risperidone on isolated microsomes of rat liver. Methods: Its biotransformation was examined using isolated microsomes derived from rat livers. Their separation was accomplished on Jasco RP-HPLC C-18 column (250mm x 4.6mm x 5µm) using methanol: 50mM Potassium dihydrogen phosphate (50:50 %v/v) mobile phase, detected at a wavelength of 280nm. Results: In vitro metabolism of RIS was investigated using the cytochrome P450 (CYP450) enzymes supplemented with an NADPH-generating system. Incubation of RIS with rat liver microsomes resulted in the formation of 2 major hydroxy metabolites. Conclusion: Formation of all the metabolites is correlated with Phase I biotransformation CYP enzyme subfamilies. The method was extended to LC-MS for further characterization of the metabolites using standards and the probable metabolites were proposed.

Indian Journal of Pharmaceutical Sciences, 2000

Bioorganic chemistry, 2014

Novel thiosemicarbazide derivatives were synthesised and evaluated for their anticonvulsant activ... more Novel thiosemicarbazide derivatives were synthesised and evaluated for their anticonvulsant activity and neurotoxicity. Anticonvulsant activity was done for grand mal and petit mal types of epilepsies by maximal electroshock (MES) and pentylenetetrazol (PTZ) induced convulsions methods respectively. Rotarod test was done to determine neurotoxicity. Amongst synthesised compounds, N-(4-bromophenyl)2-[(2-phenylhydrazinyl) carbonothioyl] hydrazinecarbothioamide (5e) is a broad-spectrum anticonvulsant agent since it was active in both (MES) and (PTZ) induced seizure models with no neurotoxicity and N,N-(bis(chlorophenyl)hydrazine-1,2-dicarbothoamide (5g) acts as a selective agent for grand mal epilepsy.

International Journal of Green Pharmacy, 2008

Tridax procumbens Linn, commonly known as Ekdandi and Mexican Daisy, is a native of tropical Amer... more Tridax procumbens Linn, commonly known as Ekdandi and Mexican Daisy, is a native of tropical America. It also grows wildly in tropical Africa, Asia and Australia and is available in all seasons and in most parts of the country (The Wealth of India, 1985). It is a hardy perennial herb ...

YAKUGAKU ZASSHI, 2008

The transdermal matrixˆlms of metoprolol tartrate (MT) were prepared by casting on mercury substr... more The transdermal matrixˆlms of metoprolol tartrate (MT) were prepared by casting on mercury substrate employing diŠerent ratios of polymers, ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP), using dibutyl phthalate (DBT) as a plasticizer. Four formulations were prepared. Formulations MF-1, MF-2, MF-3 and MF-4 were composed of EC and PVP in the following ratios: 4.5：0.5, 4：1, 3：2 and 2：3 respectively. The formulations were subjected to various physical characterization studies namely, thickness, weight variation, drug content, moisture uptake, in vitro drug release and in vitro skin permeation. The in vitro permeation studies were carried out across excised porcine ear skin using Franz diŠusion cell. Cumulative amounts of the drug released in 24 hours from the four formulations were 69.58％, 96.13％, 98.85％ and 99.60％, respectively. Corresponding values for the cumulated amounts of drug permeated across the porcine skin for the above matrixˆlms were 124.38, 153.22, 156.46 and 163.25 mg/cm 2 respectively. Byˆtting the data into zero order,ˆrst order and Higuchi model, it was concluded that drug release from matrixˆlms followed Higuchi model (r 2 ＝0.9147 0.9823), and the mechanism of release was diŠusion mediated. Based on the physical evaluation, in vitro drug release & permeation characteristics, it was concluded that for potential therapeutic use, monolithic drug matrixˆlms MF-3, composed of EC: PVP (3：2), may be suitable for the development of a transdermal drug delivery system of MT.

international journal of chemical sciences, 2009

An estimate of time to reach maximum plasma concentration (tmax) is of paramount importance in as... more An estimate of time to reach maximum plasma concentration (tmax) is of paramount importance in assessing the efficacy of drugs used to treat acute conditions like pain and insomnia, which can be treated by a single dose. This study was conducted to develop Quantitative Structure Pharmacokinetic Relationship (QSPR) for the prediction of tmax in men for congeneric series of 24 quinolone drugs, using computer assisted Hansch approach. The QSPR correlations were duly analyzed using a battery of apt statistical procedures and validated using leave-one-out (LOO) approach. Analysis of several hundreds of QSPR correlations developed in this study revealed high degree of cross-validated coefficients (Q2) using LOO method (p<0.001). The overall predictability was found to be high (R2 = 0.9147 F=33.96 S2=0.0748, Q2=0.8046 p<0.001). Both logarithmic transform and inverse transform of the tmax value resulted in decrease in correlation coefficient (for Log tmax, R2= 0.8636 and for 1/tmax, R2= 0.8701). Topological and electrostatic parameters were found to primarily ascribe the variation in tmax. The results indicate the involvement of dissolution rate limited absorption rather than permeation limited, as hardly any dependence on Log P was observed.

Research Journal of Pharmacy and Technology, Jun 28, 2008

Indian Journal of Pharmaceutical Sciences, 2000

Bioorganic Chemistry, Jul 1, 2022

Thiosemicarbazides (TSCs), dithiocarbamates (DTCs) and their molecular conjugates are promising d... more Thiosemicarbazides (TSCs), dithiocarbamates (DTCs) and their molecular conjugates are promising drug targets. However, hybrids of DTCs with TSCs themselves are rarely investigated. Thus, studies were initiated to synthesize novel system derived from TSC-DTCs to examine their pharmacological applications. The targeted conjugates were designed and synthesized from aryl TSC and aryl DTCs in moderate to good yields. The structures of synthesized compounds were confirmed through FT-IR, 1 H NMR, 13 C NMR and mass spectrometry. The conjugates have been tested for antioxidant and anticancer activities. The in vitro antioxidant activity was performed using 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging assay, hydrogen peroxide scavenging assay and nitric oxide assay and was also compared with aryl DTCs and aryl TSCs to explore potential of newly synthesized hybrids. The preliminary anticancer screening for cytotoxicity was performed using brine shrimp lethality bioassay using Artemia salina shrimps. Anticancer screening was determined against NCI 60 human tumor cell lines at NCI, USA. The results revealed that, newly synthesized hybrids are more active as compared to aryl DTCs and aryl TSCs. Among the tested conjugates for antioxidant screening, 3b was found to be more active than the standard ascorbic acid. The IC 50 value of 3b were 8.96 ± 0.089, 10.7 ± 0.016 and 12.29 ± 0.086 μg/ml for DPPH, hydrogen peroxide scavenging assay and nitric oxide assay respectively, whereas IC 50 values for standard were 11.75 ± 0.015, 12.03 ± 0.107 and 16.66 ± 0.242 μg/ml respectively. Since hybrids are more active than aryl DTCs and aryl TSCs, only newly synthesized hybrids were screened for anticancer potential. For cytotoxicity screening, compound 3b was found to be most active among synthesized conjugates with LD 50 value of 33.86 μg/ ml. For anticancer screening, the compounds 3c and 3d were found to be potent among synthesized series with percent growth inhibition of 22 to 44% when screened against colon cancer cell lines whereas, compound 3b showed growth inhibition of 40% for selective leukemia cell line, K-562. The compounds 3b, 3c and 3d with strong electron-withdrawing groups were found to be the most active antioxidant and anticancer agents among the synthesized conjugates.

Indian Journal of Pharmaceutical Sciences, 2001

A new simple and sensitive spectrophotometric method in the UV region has been developed for the ... more A new simple and sensitive spectrophotometric method in the UV region has been developed for the simultaneous determination of mefenamic acid and paracetamol in bulk and in dosage forms. Mefenamic acid shows three absorbance maxima at 219,284 and 336 nm and paracetamol shows a single absorbance maximum at 257 nm in 0.1N sodium hydroxide. Absorbance corrected for interference was used for estimation. Both these drugs obey Beer's law In the concentration ranges used in this method. The method has been validated statistically and by recovery studies.

Journal of Current Pharma Research, 2013

Currently, inflammatory diseases are being treated with drugs most of which have side effects. Th... more Currently, inflammatory diseases are being treated with drugs most of which have side effects. There is a need to develop newer analogs especially from phytochemical sources that have lesser or no side effects. Hence, we thought it worthwhile to isolate phytosterols from leaves of Tridax procumbens plant, prepare their semisynthetic derivatives and evaluate them for anti-inflammatory activity. Column chromatography and preparative TLC were employed to isolate β-sitosterol and stigmasterol. Their acetylated derivatives were prepared using conventional organic reactions. The compounds were evaluated for invivo anti-inflammatory activity using carrageenan-induced paw oedema method in rats. Results revealed that both β-sitosterol and stigmasterol have significant anti-inflammatory activity viz., 65% and 67%; respectively with standard diclofenac exhibiting 68% inhibition. Derivatives betasitosteryl acetate and stigmasteryl acetate showed 61% and 62% inhibition; respectively. Thus, phytosterols and derivatives of Tridax procumbens leaves can be used as leads to make future drug candidates to treat inflammatory conditions.

Cyclic peptides have emerged as an important class of organic compounds with potent biological ac... more Cyclic peptides have emerged as an important class of organic compounds with potent biological activities like antifungal, antibacterial, anthelmintic, antineoplastic, insecticidal, anti-inflammatory, melanin production inhibitory activities. The inherent medicinal properties of cyclic peptides promoted scientists to isolate these compounds from natural sources. Since only minute quantities are obtained from natural sources, attempts have been made for the synthesis of these compounds in laboratories and biological screening of these compounds gave good results. Number of modifications has been done in the structure of basic cyclic peptides in order to increase their biological activities. Thus there is wide scope for synthesis of these peptides and their derivatives to explore more potent biodynamic molecules. The present review encompasses the idea about the various peptide molecules and their derivatives which have been synthesized in the laboratory and had shown potent biologica...

Green methods such as microwave technique and grinding technique have been found superior over th... more Green methods such as microwave technique and grinding technique have been found superior over the conventional method in view of reaction time and energy requirement. Pyrazoline derivatives , 2a-i and 3a-i, were synthesized both conventional heating and by microwave irradiation, the synthesized compounds were characterized by 1H NMR, 13C NMR, IR and mass spectral analyses. They were screened for their in vitro anti-inflammatory, antimicrobial and antioxidant activities. Antimicrobial activity was performed by Agar plate method and 2d & 2e were active against Gram negative bacteria E. coli and S. aureus, 3c and 3g showed antioxidant activity (IC50=48.13 and 46.03μg/ml),3c shows respectively anti-inflammatory activity at (EC50= 11.00±1.26 µg/mL) 3c ,3d and 3e showed good anti-inflammatory activity at concentration (EC50= 11.70±0.98 µg/mL) & 11.70±0.98 µg/mL respectively.

Green methods such as microwave technique and grinding technique has been found superior over the... more Green methods such as microwave technique and grinding technique has been found superior over the conventional method in view of reaction time and energy requirement. Comp research (2a-i), (3a-i) have been characterized by 1H NMR, 13C NMR, IR and mass spectral analyses. They were screened for their in vitro anti-inflammatory, antimicrobial and in vitro antioxidant activities. Antimicrobial activity was performed by Agar plate method and comp. 2d & 2e a active against gram negative bacteria E. coli and S. aureus, the comp. 3c and 3g show antioxidant activity as (IC50 = 48.13 and 46.03µg/ml), Comp’ 3c shows respectively anti-inflammatory activity at (EC50 = 11.00 ± 1.26 µg/mL). Comp. ,3c ,3d and 3e showed good anti-inflammatory activity at concentration (EC50 = 11.70 ± 0.98 µg/mL) & 11.70 ± 0.98 µg/mL respectively.

Ammannia baccifera Linn, (family Lythraceae), traditionally it is used as cooling appetizer, rubi... more Ammannia baccifera Linn, (family Lythraceae), traditionally it is used as cooling appetizer, rubifacient, laxative, stomachic, diuretic, aphrodisiac and lithotriptic also reported as posses antityphoid and antitubercular.The present study was investigated to evaluate in vitro antimicrobial activity of aqueous, methanolic, hexane extracts against bacteria Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus and against the fungi Candida albicans,Kluyuviromyces mamlamus.The pathogens were tested by disc diffusion assay method, and An attempt has been made to compare the activity of extracts with standard antibiotics against selected pathogen and all the extracts exhibited significant activity.

Bioorganic & Medicinal Chemistry, 2005

In view of obtaining some potential antibacterial compounds, we have described synthesis of some ... more In view of obtaining some potential antibacterial compounds, we have described synthesis of some chloroaryloxyalkyl imidazole and benzimidazole derivatives. The relevant step in the synthetic sequence was the initial condensation of 4-chloro or 2,4-dichlorophenol with 1, n-dibromoalkanes (n=2, 4, 5) to provide compounds 3a-f in sufficient yields. The subsequent condensation of 3a-f with some imidazole derivatives and benzimidazole afforded products 4a-l and 5a-e in good yields. Some of compounds 4a-l as well as 5a-e were tested in vitro against Salmonella typhi O-901 and Staphylococcus aureus A 15091. Compounds 4a and 4c showed considerable bactericidal activities against tested bacteria. Compound 4b showed significant activity against S. aureus A 15091 but was inactive against S. typhi O-901. Other compounds showed intermediate activities against S. aureus A 15091 but most of them were inactive against S. typhi O-901. Semiempirical AM1 calculations showed that negative electrostatic potentials around oxygen of the phenoxy and nitrogen of the imidazole moieties have direct effect on the antibacterial activity towards S. aureus A 15091. In QSAR analysis, different electronic, topologic, functional groups and physicochemical descriptors were calculated for each molecule and a three parametric equation was found between the logMIC and HOMO energy, hydration energy and number of primary carbon atoms of the molecules.

Indian Journal of Pharmaceutical Sciences, 2011

The aim of this study was to evaluate the binding efficiency of mucilage extracted from Dioscorea... more The aim of this study was to evaluate the binding efficiency of mucilage extracted from Dioscorea alata(water yam). The sustained release matrix tablet of Isoniazid was prepared by wet granulation technique using Dioscorea alata Linn. polysaccharide. The polysaccharide was extracted from the tuber via maceration method and evaluated for their color, viscosity and pH.The prepared tablet was evaluated for their hardness, friability, drug content,swelling studies and In vitro dissolution rate. Optimized Formulation F2 and F3 was exhibited satisfactory results as 95 % and 91 % in 12 hrs.whereas formulation F-5 shows 85 % of drug release in 12 hrs. The drug release from the tablet was sustained and non-Fickian transport of drug from the tablet was confirmed. Using Higuchi's Model and the Korsmeyer equation, the drug release mechanism from the sustained release tablets was found to be Anomalous (non-Fickian) diffusion. Compatibility study confirmed that interactions do not exist between the drug and polymer.

Indian Journal of Pharmaceutical Sciences, 2005

A rapid, selective and precise HPLC method for quantification of ofloxacin in tablets has been de... more A rapid, selective and precise HPLC method for quantification of ofloxacin in tablets has been developed. The chromatographic resolution of ofloxacin was achieved using acetonitrile:0.1%v/v triethylamine (20:80, pH-4.0) as the mobile phase, in an isocratic run on a chromatographic system (Waters) equipped with Waters 600 pump controller, 2487 dual I» absorbance detector, Waters32 millennium chromatography manager software and C8 kromasil 5I¼ (4.6x150 mm) column. The flow rate was 1 ml/min and ofloxacin was monitored spectrophotometrically at 280 nm. Ornidazole was used as an internal standard.

RESEARCH AND EDUCATION IN INDIAN …, 2011

Bauhinia variegata Linn (BV), commonly known as Raktkanchan is a medium sized deciduous tree foun... more Bauhinia variegata Linn (BV), commonly known as Raktkanchan is a medium sized deciduous tree found throughout India and traditionally used to cure variety of ailments. In Ayurveda, the plant is documented to be useful as rasayana. The present investigation was planned to evaluate immunomodulatory potential of aqueous (BVA) and ethanol (BVE) extracts of stem bark of BV on neutrophil phagocytic function. The various concentrations (25, 50 and 100 mg/ml) of both the extracts were subjected to study their effects on different in vitro methods of Phagocytosis such as neutrophil locomotion and chemotaxis, immunostimulant activity by Phagocytosis of killed Candida albicans and qualitative nitro blue tetrazolium test using human neutrophils. The results of this preliminary study shown that both the extracts of BV possess stimulatory effect on chemotactic, phagocytic and intracellular killing potency of human neutrophils at the concentration range of 25-100 mg/ml. However, significant activity was revealed by BVE at highest concentration of 100 mg/ml in all the parameters studied. These results suggest that stem bark extracts of B.variegata possess immunomodulatory activity and justifies its use in Ayurveda as rasayana.

Indian Journal of Pharmaceutical Education and Research, 2019

Objective: The objective of present research work is to study in vitro metabolism of risperidone ... more Objective: The objective of present research work is to study in vitro metabolism of risperidone on isolated microsomes of rat liver. Methods: Its biotransformation was examined using isolated microsomes derived from rat livers. Their separation was accomplished on Jasco RP-HPLC C-18 column (250mm x 4.6mm x 5µm) using methanol: 50mM Potassium dihydrogen phosphate (50:50 %v/v) mobile phase, detected at a wavelength of 280nm. Results: In vitro metabolism of RIS was investigated using the cytochrome P450 (CYP450) enzymes supplemented with an NADPH-generating system. Incubation of RIS with rat liver microsomes resulted in the formation of 2 major hydroxy metabolites. Conclusion: Formation of all the metabolites is correlated with Phase I biotransformation CYP enzyme subfamilies. The method was extended to LC-MS for further characterization of the metabolites using standards and the probable metabolites were proposed.

Indian Journal of Pharmaceutical Sciences, 2000

Bioorganic chemistry, 2014

Novel thiosemicarbazide derivatives were synthesised and evaluated for their anticonvulsant activ... more Novel thiosemicarbazide derivatives were synthesised and evaluated for their anticonvulsant activity and neurotoxicity. Anticonvulsant activity was done for grand mal and petit mal types of epilepsies by maximal electroshock (MES) and pentylenetetrazol (PTZ) induced convulsions methods respectively. Rotarod test was done to determine neurotoxicity. Amongst synthesised compounds, N-(4-bromophenyl)2-[(2-phenylhydrazinyl) carbonothioyl] hydrazinecarbothioamide (5e) is a broad-spectrum anticonvulsant agent since it was active in both (MES) and (PTZ) induced seizure models with no neurotoxicity and N,N-(bis(chlorophenyl)hydrazine-1,2-dicarbothoamide (5g) acts as a selective agent for grand mal epilepsy.

International Journal of Green Pharmacy, 2008

Tridax procumbens Linn, commonly known as Ekdandi and Mexican Daisy, is a native of tropical Amer... more Tridax procumbens Linn, commonly known as Ekdandi and Mexican Daisy, is a native of tropical America. It also grows wildly in tropical Africa, Asia and Australia and is available in all seasons and in most parts of the country (The Wealth of India, 1985). It is a hardy perennial herb ...

YAKUGAKU ZASSHI, 2008

The transdermal matrixˆlms of metoprolol tartrate (MT) were prepared by casting on mercury substr... more The transdermal matrixˆlms of metoprolol tartrate (MT) were prepared by casting on mercury substrate employing diŠerent ratios of polymers, ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP), using dibutyl phthalate (DBT) as a plasticizer. Four formulations were prepared. Formulations MF-1, MF-2, MF-3 and MF-4 were composed of EC and PVP in the following ratios: 4.5：0.5, 4：1, 3：2 and 2：3 respectively. The formulations were subjected to various physical characterization studies namely, thickness, weight variation, drug content, moisture uptake, in vitro drug release and in vitro skin permeation. The in vitro permeation studies were carried out across excised porcine ear skin using Franz diŠusion cell. Cumulative amounts of the drug released in 24 hours from the four formulations were 69.58％, 96.13％, 98.85％ and 99.60％, respectively. Corresponding values for the cumulated amounts of drug permeated across the porcine skin for the above matrixˆlms were 124.38, 153.22, 156.46 and 163.25 mg/cm 2 respectively. Byˆtting the data into zero order,ˆrst order and Higuchi model, it was concluded that drug release from matrixˆlms followed Higuchi model (r 2 ＝0.9147 0.9823), and the mechanism of release was diŠusion mediated. Based on the physical evaluation, in vitro drug release & permeation characteristics, it was concluded that for potential therapeutic use, monolithic drug matrixˆlms MF-3, composed of EC: PVP (3：2), may be suitable for the development of a transdermal drug delivery system of MT.