mayura kale - Academia.edu (original) (raw)
Papers by mayura kale
Der Pharmacia sinica, 2015
In the present work, we have studied group quantitative structure–activity relationship (G-QSAR) ... more In the present work, we have studied group quantitative structure–activity relationship (G-QSAR) to understand the correlation between the structures of a new emerging family of 1,2,4-triazolo [3,4-b]-1,3,4-thiadiazole derivatives and their antifungal activities. We have developed descriptive validated models, for development of newer antifungal agents containing the thiadiazole linked triazole pharmacophore. These studies have been performed on V-Life molecular design suite (MDS) software. For model validation, the dataset was divided into various training and test sets using sphere exclusion method. The developed G-QSAR models were found to be statistically significant with respect to training (r2>0.7), cross-validation (q2>0.5), and external validation (pred_r2>0.5). The developed G-QSAR model suggests that the nature of substitution on one of the aryl fragment is highly influential in determining biological activity.
Digital Chinese Medicine, 2021
Indian Journal of Pharmaceutical Sciences, 2013
The simple, selective, precise and accurate reverse-phase high-performance liquid chromatography ... more The simple, selective, precise and accurate reverse-phase high-performance liquid chromatography method was developed and validated for analysis of tadalafil in bulk and tablet dosage form. The column was Inertsil C18 (150×4.6 mm; 5 μm) in isocratic mode. The mobile phase used was phosphate buffer (10 mM, pH 3.2) and acetonitrile (50:50% v/v) at the flow rate of 1.0 ml/min with ultraviolet detection at 295 nm at ambient temperature. The retention time for tadalafil was found to be 4.01 min. Linearity was observed in the concentration range from 60 to 140 μg/ml for tadalafil with a correlation coefficient of (r2) 0.9998. The method was validated according to International Conference on Harmonisation guidelines in terms of linearity, accuracy, precision and specificity. Hence, the proposed method can be utilized for routine quality control of tadalafil in bulk and tablet dosage form.
In the present work, we have studied group quantitative structure–activity relationship (G-QSAR) ... more In the present work, we have studied group quantitative structure–activity relationship (G-QSAR) to understand the correlation between the structures of a new emerging family of 1,2,4-triazolo [3,4-b]-1,3,4-thiadiazole derivatives and their antifungal activities. We have developed descriptive validated models, for development of newer antifungal agents containing the thiadiazole linked triazole pharmacophore. These studies have been performed on V-Life molecular design suite (MDS) software. For model validation, the dataset was divided into various training and test sets using sphere exclusion method. The developed G-QSAR models were found to be statistically significant with respect to training (r2>0.7), cross-validation (q2>0.5), and external validation (pred_r2>0.5). The developed G-QSAR model suggests that the nature of substitution on one of the aryl fragment is highly influential in determining biological activity.
Indo Global Journal of Pharmaceutical Sciences, 2020
3D quantitative structure activity relationship study was performed on a series of some (2-benzyl... more 3D quantitative structure activity relationship study was performed on a series of some (2-benzylcarbamoylphenoxy)- acetic acid derivatives for treatment of chronic diabetic complications for establishing n quantitative relationship between biological activity and their physicochemical properties. Several statistical regression expressions were obtained with 3D-QSAR study using k-Nearest Neighbor (kNN) method and four statistical significant models were generated by using Sphere Exclusion method and Randon Selection Method. By kNN Sphere Exclusion Method (q2= 0.5042 , 0.6433 and pred_r2= 0.6939, 0.7115 for model 1 and 2 respectively) and kNN Randon Selection Method (q2= 0.6297, 0.7107 and pred_r2=0.8970,0.5908 for model 3,4 respectively).
Novel derivatives of 2-amino-3-cyano-14-imino-10-me thoxy-4-methylthio pyrimido [2,1-b] pyrazolo ... more Novel derivatives of 2-amino-3-cyano-14-imino-10-me thoxy-4-methylthio pyrimido [2,1-b] pyrazolo [4,5-d] pyrimido [2,1-b] benzothiazole 4 were synthesized from starting material 2amino-6-methoxy benzothiazole 1 and evaluated for their anti-inflammatory activity . It was concluded that some of the compounds showed excelle nt anti-inflammatory activity as compared with others.
The biological potential of various heterocyclic scaffolds draw special attention of medicinal ch... more The biological potential of various heterocyclic scaffolds draw special attention of medicinal chemists and hence exhaustive efforts are being carried out in the search of lead molecules pertaining to it. The knowledge of such biologically important heterocycles and their methods of synthesis are discussed in this review. Especially, the focus is kept on the heterocycles that are effective to treat many significant lifestyle diseases such as atherosclerosis, diabetes, ischemic heart disease, myocardial infarctions, which are strongly associated with imbalance in lipid metabolism and plasma lipoproteins. As these conditions are responsible for one-third of deaths in industrialized nations, special emphasis is given on synthesis of recently reported heterocycles possessing anti-hyperlipidemic activity. Such derivatives have been extensively studied in the past few decades. The present review includes the rigorous literature survey on the methods of preparation along with the potential...
International Journal of Pharmaceutical Sciences Review and Research, 2020
In present study various pharmacological investigation of alkaline water compiled, now days due t... more In present study various pharmacological investigation of alkaline water compiled, now days due to fast life acidity become a huge problem in metro cities which is origin for various diseases such a GERD, hypertension, skin diseases, hyperthyroidism, hyperlipidemia, cancer, diabetes etc. Various researches worked on activity of alkaline water and various clinical trials are in tunnel. Compile date elucidate the importance of alkaline water in various diseases treatments and future prospectus in clinical trials of various cancer and related diseases.
Current Computer-Aided Drug Design, 2020
Background: The computational studies on 2-phenazinamines with their protein targets have been ca... more Background: The computational studies on 2-phenazinamines with their protein targets have been carried out to design compounds with potential anticancer activity and selectivity over specific BCR-ABL Tyrosine kinase. Methods: This has been achieved through G-QSAR and molecular docking studies. Computational chemistry was done by using VLife MDS 4.3 and Autodock 4.2. 2D and structures of ligands were drawn by using Chemdraw 2D Ultra 8.0 and were converted into 3D. These were optimized by using semi-empirical method called MOPAC. The protein structure was downloaded as PDB file from RCSC protein data bank. PYMOL was used for studying the binding interactions. The G-QSAR models generated were found to possess training (r2=0.8074), cross-validation (q2=0.6521), and external validation (pred_r2=0.5892) which proved their statistical significance. Accordingly, the newly designed series of 2-phenazinamines viz., 3-chloro-4-aryl-1-(phenazin-7-yl) azetidin-2-ones (4a-4e) were subjected to we...
Current Computer-Aided Drug Design, 2018
There has been a rapid surge in the research and exchange of ideas in various areas of chemistry ... more There has been a rapid surge in the research and exchange of ideas in various areas of chemistry such as organic, pharmaceutical, analytical, and medicinal chemistry. It is well recognized that heterocycles are vital components of many biochemical processes. Pharma industry comprises more than 75% of top selling drugs that are of heterocyclic origin. Among many diseases, cancer can be considered to be a dreaded disease that has overtaken the masses across the globe. Hence, there has been a need to develop drugs that are less toxic and do not provide resistance in the long run. Thus, this need-based development of anticancer drugs through the use of heterocycles has gained its pace since last two decades and there has been a gush among the researchers to apply various approaches in designing anticancer molecules. More specifically, research is being targeted on the utilization of molecular modeling techniques for developing new anticancer agents specifically targeting various cancer cell lines, specific enzymes and tissues. Some of the important and conclusive findings using this approach have been presented in this review.
Journal of Current Pharma Research, 2014
Various heterocyclic scaffolds have drawn special attention of medicinal chemists and hence, exte... more Various heterocyclic scaffolds have drawn special attention of medicinal chemists and hence, extensive efforts are being carried out in search of lead molecules related to it. Benzimidazole is an important pharmacophore owing to its inherent properties and therapeutic actions. These exhibit many biological activities like anticancer, anticonvulsant, antiHIV, antimicrobial and many more. Such biological applications of benzimidazole derivatives have attracted attention and stimulated new search for its novel derivatives with improved biological activities and these are being extensively studied. The present review includes rigorous literature survey on the search of biologically active benzimidazole ring linked and fused with other heteroaromatic systems.
Eurasian Journal of Analytical Chemistry, 2016
A new high performance liquid chromatography method was developed and validated for the quantitat... more A new high performance liquid chromatography method was developed and validated for the quantitation of Cilnidipine and Valsartan in pharmaceutical formulations. Determination was performed using an ODS C18, 250mm x 4.6mm, 5μm column, a mobile phase containing Methanol: Water (85:15) pH 3 adjusts with ortho-phosphoric acid in isocratic flow rate 1.0 mLmin-1. The method was validated with respect to linearity, precision, robustness, and accuracy. The calibration graphs ranged from 1-5 μg/mL in Cilnidipine and 8-40 μg/mL Valsartan Intra-and interday relative standard deviation values for the standard solutions were 0.5%, 1.64% and 0.22%, 1.62 %. Robustness of relative standard deviation values was 0.334, 0.101 respectively. Total recoveries of Cilnidipine and Valsartan from the laboratory prepared mixtures were 98.94 % and 99.04 % respectively.
![Research paper thumbnail of G-QSAR of Novel 2-{[2-(1H-imidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole Derivatives](https://attachments.academia-assets.com/116950805/thumbnails/1.jpg)
](Chemical Science Transactions, 2014
In the present work, we have applied group quantitative structure-activity relationships (G-QSAR)... more In the present work, we have applied group quantitative structure-activity relationships (G-QSAR) for exploring the relationship between the structures of a new emerging family of 2-{[2-(1Himidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole derivatives and their antiprotozoal activities. We have developed descriptive models, in order to aid in further optimization and development of newer antiprotozoal agents containing the benzimidazole pharmacophore. G-QSAR was performed on VLife molecular design suite (MDS) 4.5 version software. The predictive power of the QSAR was checked through the cross validation technique and also by leaving some compounds as part of external test set
Bangladesh Journal of Pharmacology, 2017
The methanolic extract of Alysicarpus vaginalis was selected for fractionation due to its known r... more The methanolic extract of Alysicarpus vaginalis was selected for fractionation due to its known reported biological activity. The four fractions were separated and subjected for in vitro antimitotic and anti-proliferative assays along with anti-cancer activity on two human cancers cell lines (SK-MEL-2 and Hep-G2). The antimicrobial potential of fractions had been evaluated against bacteria and fungi. From all fractions, acetone and n-butanol fractions were effective against the cell lines. They show strong inhibitory action with mitotic index 6.2 and 8.4 mg/mL and IC50 values of anti-proliferative assay in between 19.7 to 14.2 mg/mL respectively, which was found to be comparable to the standard methothrexate 5.9 mg/mL and 13.2 mg/mL respectively. In antimicrobial activity, the zone of inhibition had been observed in the range of 12-27 mm and MIC value was found in the range of 0.2-0.1 mg/mL. The acetone fraction was found to be most active against fungi, and E. coli whereas chlorofo...
Advanced Science Letters, 2016
Journal of Chemical & Engineering Data, 2015
Models for predicting the solubility of drugs in monosolvents and their mixtures have a practical... more Models for predicting the solubility of drugs in monosolvents and their mixtures have a practical importance in design and development of new products in pharmaceutical industries. Thus, present investigation pertains to the utility of a correlative model for solubility prediction of etoricoxib (ETR). The molar solubilities of ETR in a number of monosolvents and various mass fractions of their binary aqueous solvent mixtures were determined using the shakeflask method at 298.2 K. Densities of ETR saturated solutions in the monosolvents and their binary solvent mixtures were measured and then correlated using a well-established method proposed by Jouyban and Acree. Overall mean percentage deviations (OMPDs) between experimental and predicted values were 3.4 % for the molar solubilities and 0.1 % for the densities of the saturated solutions.
International Journal of Applied Pharmaceutics, 2015
Human body is known to experience positive stress that keeps it vigilant and protects it from bio... more Human body is known to experience positive stress that keeps it vigilant and protects it from biological and physical threats. This stress turns negative when a person is confronted with continuous challenges. Also, stress and nutrition have always run in synergism with each other. Nutritional value of a person's diet depends on the overall mixture or balance of food that is eaten over a period of time, as well as on the needs of the individual. The body relies on obtaining its anti-oxidants from food and other supplements. These nutritional requirements of antioxidants are enormously altered in diseased conditions. In view of the immense medicinal importance of antioxidants, an effort has been made in this article to bring together information about the role of nutrition and antioxidants such as carotenoids, vitamins, some important minerals in combating free radical generation and in general, boosting normal immune mechanisms. The present review is an attempt to generate interest in the scientific fraternity of their immense potential in preventing and treating several common diseases.
International Journal of Pharmacy and Pharmaceutical Sciences, 2014
There is a growing interest towards the development of new antibiotics from last decades due to e... more There is a growing interest towards the development of new antibiotics from last decades due to emergence of newer pathogenic bacterial strains with high resistance to powerful antibiotics of last resort. This has caused decline in research for developing newer antibacterial agents. Hence, there is continuous need to develop newer antibiotics that interact with essential mechanisms in bacteria. Recently, enzymes responsible for bio synthesis of the essential amino acid lysine in bacteria have been targeted and it has augmented interest to develop novel antibiotics and to enhance lysine yields in over-producing organisms. Peptidoglycan layer consists of a beta-1,4-linked polysaccharide of alternating N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAM) sugar units, cross linked by short pentapeptide (muramyl residues) side chain of general structure L-Ala-g-D-Glu-X-D-Ala-D-Ala, where X is either L-Lysine or meso-DAP. Formation of the cross-links makes bacterial cell wall resistant to lysis by intracellular osmotic pressure. Compounds which inhibit lysine or DAP biosynthesis could therefore be very effective antibiotics and novel targets. Lysine is a constituent in gram-positive bacteria while meso-DAP occurs in gram negative ones. In this review, substrate-based inhibitors of enzymes in the DAP pathway and inhibitors that allow better understanding of enzymology of the targets and provide insight for design of new inhibitors have been discussed. Resistant bacterial strains can be inhibited by using synthetic enzyme inhibitors of DAP pathway that are less toxic to mammals. Newer antimicrobial drugs can be thus developed by targeting the enzymes involved in this pathway.
Current Organic Synthesis, 2015
Substantial attention has been given in developing novel heterocyclic compounds as these have bee... more Substantial attention has been given in developing novel heterocyclic compounds as these have been found to exhibit varied biological activities. Benzothiazoles belong to one of the special categories of heterocyclic compounds with a wide range of biological activities such as antimicrobial, antitumor, antidiabetic, antitubercular, antimalarial, anticonvulsant, anthelmintic, analgesic, antiinflammatory and many more. These compounds have been serving as leads for researchers who are actively involved in synthesizing and evaluating their biological activities. Such an extensive work has stimulated further development of new benzothiazole derivatives with enhanced biological activities. This review focuses on the various approaches on the synthesis of benzothiazole derivatives viz., conventional, green, combinatorial and microwave-assisted methods. It also highlights various biological activities of the currently synthesized benzothiazoles.
Der Pharmacia sinica, 2015
In the present work, we have studied group quantitative structure–activity relationship (G-QSAR) ... more In the present work, we have studied group quantitative structure–activity relationship (G-QSAR) to understand the correlation between the structures of a new emerging family of 1,2,4-triazolo [3,4-b]-1,3,4-thiadiazole derivatives and their antifungal activities. We have developed descriptive validated models, for development of newer antifungal agents containing the thiadiazole linked triazole pharmacophore. These studies have been performed on V-Life molecular design suite (MDS) software. For model validation, the dataset was divided into various training and test sets using sphere exclusion method. The developed G-QSAR models were found to be statistically significant with respect to training (r2>0.7), cross-validation (q2>0.5), and external validation (pred_r2>0.5). The developed G-QSAR model suggests that the nature of substitution on one of the aryl fragment is highly influential in determining biological activity.
Digital Chinese Medicine, 2021
Indian Journal of Pharmaceutical Sciences, 2013
The simple, selective, precise and accurate reverse-phase high-performance liquid chromatography ... more The simple, selective, precise and accurate reverse-phase high-performance liquid chromatography method was developed and validated for analysis of tadalafil in bulk and tablet dosage form. The column was Inertsil C18 (150×4.6 mm; 5 μm) in isocratic mode. The mobile phase used was phosphate buffer (10 mM, pH 3.2) and acetonitrile (50:50% v/v) at the flow rate of 1.0 ml/min with ultraviolet detection at 295 nm at ambient temperature. The retention time for tadalafil was found to be 4.01 min. Linearity was observed in the concentration range from 60 to 140 μg/ml for tadalafil with a correlation coefficient of (r2) 0.9998. The method was validated according to International Conference on Harmonisation guidelines in terms of linearity, accuracy, precision and specificity. Hence, the proposed method can be utilized for routine quality control of tadalafil in bulk and tablet dosage form.
In the present work, we have studied group quantitative structure–activity relationship (G-QSAR) ... more In the present work, we have studied group quantitative structure–activity relationship (G-QSAR) to understand the correlation between the structures of a new emerging family of 1,2,4-triazolo [3,4-b]-1,3,4-thiadiazole derivatives and their antifungal activities. We have developed descriptive validated models, for development of newer antifungal agents containing the thiadiazole linked triazole pharmacophore. These studies have been performed on V-Life molecular design suite (MDS) software. For model validation, the dataset was divided into various training and test sets using sphere exclusion method. The developed G-QSAR models were found to be statistically significant with respect to training (r2>0.7), cross-validation (q2>0.5), and external validation (pred_r2>0.5). The developed G-QSAR model suggests that the nature of substitution on one of the aryl fragment is highly influential in determining biological activity.
Indo Global Journal of Pharmaceutical Sciences, 2020
3D quantitative structure activity relationship study was performed on a series of some (2-benzyl... more 3D quantitative structure activity relationship study was performed on a series of some (2-benzylcarbamoylphenoxy)- acetic acid derivatives for treatment of chronic diabetic complications for establishing n quantitative relationship between biological activity and their physicochemical properties. Several statistical regression expressions were obtained with 3D-QSAR study using k-Nearest Neighbor (kNN) method and four statistical significant models were generated by using Sphere Exclusion method and Randon Selection Method. By kNN Sphere Exclusion Method (q2= 0.5042 , 0.6433 and pred_r2= 0.6939, 0.7115 for model 1 and 2 respectively) and kNN Randon Selection Method (q2= 0.6297, 0.7107 and pred_r2=0.8970,0.5908 for model 3,4 respectively).
Novel derivatives of 2-amino-3-cyano-14-imino-10-me thoxy-4-methylthio pyrimido [2,1-b] pyrazolo ... more Novel derivatives of 2-amino-3-cyano-14-imino-10-me thoxy-4-methylthio pyrimido [2,1-b] pyrazolo [4,5-d] pyrimido [2,1-b] benzothiazole 4 were synthesized from starting material 2amino-6-methoxy benzothiazole 1 and evaluated for their anti-inflammatory activity . It was concluded that some of the compounds showed excelle nt anti-inflammatory activity as compared with others.
The biological potential of various heterocyclic scaffolds draw special attention of medicinal ch... more The biological potential of various heterocyclic scaffolds draw special attention of medicinal chemists and hence exhaustive efforts are being carried out in the search of lead molecules pertaining to it. The knowledge of such biologically important heterocycles and their methods of synthesis are discussed in this review. Especially, the focus is kept on the heterocycles that are effective to treat many significant lifestyle diseases such as atherosclerosis, diabetes, ischemic heart disease, myocardial infarctions, which are strongly associated with imbalance in lipid metabolism and plasma lipoproteins. As these conditions are responsible for one-third of deaths in industrialized nations, special emphasis is given on synthesis of recently reported heterocycles possessing anti-hyperlipidemic activity. Such derivatives have been extensively studied in the past few decades. The present review includes the rigorous literature survey on the methods of preparation along with the potential...
International Journal of Pharmaceutical Sciences Review and Research, 2020
In present study various pharmacological investigation of alkaline water compiled, now days due t... more In present study various pharmacological investigation of alkaline water compiled, now days due to fast life acidity become a huge problem in metro cities which is origin for various diseases such a GERD, hypertension, skin diseases, hyperthyroidism, hyperlipidemia, cancer, diabetes etc. Various researches worked on activity of alkaline water and various clinical trials are in tunnel. Compile date elucidate the importance of alkaline water in various diseases treatments and future prospectus in clinical trials of various cancer and related diseases.
Current Computer-Aided Drug Design, 2020
Background: The computational studies on 2-phenazinamines with their protein targets have been ca... more Background: The computational studies on 2-phenazinamines with their protein targets have been carried out to design compounds with potential anticancer activity and selectivity over specific BCR-ABL Tyrosine kinase. Methods: This has been achieved through G-QSAR and molecular docking studies. Computational chemistry was done by using VLife MDS 4.3 and Autodock 4.2. 2D and structures of ligands were drawn by using Chemdraw 2D Ultra 8.0 and were converted into 3D. These were optimized by using semi-empirical method called MOPAC. The protein structure was downloaded as PDB file from RCSC protein data bank. PYMOL was used for studying the binding interactions. The G-QSAR models generated were found to possess training (r2=0.8074), cross-validation (q2=0.6521), and external validation (pred_r2=0.5892) which proved their statistical significance. Accordingly, the newly designed series of 2-phenazinamines viz., 3-chloro-4-aryl-1-(phenazin-7-yl) azetidin-2-ones (4a-4e) were subjected to we...
Current Computer-Aided Drug Design, 2018
There has been a rapid surge in the research and exchange of ideas in various areas of chemistry ... more There has been a rapid surge in the research and exchange of ideas in various areas of chemistry such as organic, pharmaceutical, analytical, and medicinal chemistry. It is well recognized that heterocycles are vital components of many biochemical processes. Pharma industry comprises more than 75% of top selling drugs that are of heterocyclic origin. Among many diseases, cancer can be considered to be a dreaded disease that has overtaken the masses across the globe. Hence, there has been a need to develop drugs that are less toxic and do not provide resistance in the long run. Thus, this need-based development of anticancer drugs through the use of heterocycles has gained its pace since last two decades and there has been a gush among the researchers to apply various approaches in designing anticancer molecules. More specifically, research is being targeted on the utilization of molecular modeling techniques for developing new anticancer agents specifically targeting various cancer cell lines, specific enzymes and tissues. Some of the important and conclusive findings using this approach have been presented in this review.
Journal of Current Pharma Research, 2014
Various heterocyclic scaffolds have drawn special attention of medicinal chemists and hence, exte... more Various heterocyclic scaffolds have drawn special attention of medicinal chemists and hence, extensive efforts are being carried out in search of lead molecules related to it. Benzimidazole is an important pharmacophore owing to its inherent properties and therapeutic actions. These exhibit many biological activities like anticancer, anticonvulsant, antiHIV, antimicrobial and many more. Such biological applications of benzimidazole derivatives have attracted attention and stimulated new search for its novel derivatives with improved biological activities and these are being extensively studied. The present review includes rigorous literature survey on the search of biologically active benzimidazole ring linked and fused with other heteroaromatic systems.
Eurasian Journal of Analytical Chemistry, 2016
A new high performance liquid chromatography method was developed and validated for the quantitat... more A new high performance liquid chromatography method was developed and validated for the quantitation of Cilnidipine and Valsartan in pharmaceutical formulations. Determination was performed using an ODS C18, 250mm x 4.6mm, 5μm column, a mobile phase containing Methanol: Water (85:15) pH 3 adjusts with ortho-phosphoric acid in isocratic flow rate 1.0 mLmin-1. The method was validated with respect to linearity, precision, robustness, and accuracy. The calibration graphs ranged from 1-5 μg/mL in Cilnidipine and 8-40 μg/mL Valsartan Intra-and interday relative standard deviation values for the standard solutions were 0.5%, 1.64% and 0.22%, 1.62 %. Robustness of relative standard deviation values was 0.334, 0.101 respectively. Total recoveries of Cilnidipine and Valsartan from the laboratory prepared mixtures were 98.94 % and 99.04 % respectively.
Chemical Science Transactions, 2014
In the present work, we have applied group quantitative structure-activity relationships (G-QSAR)... more In the present work, we have applied group quantitative structure-activity relationships (G-QSAR) for exploring the relationship between the structures of a new emerging family of 2-{[2-(1Himidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole derivatives and their antiprotozoal activities. We have developed descriptive models, in order to aid in further optimization and development of newer antiprotozoal agents containing the benzimidazole pharmacophore. G-QSAR was performed on VLife molecular design suite (MDS) 4.5 version software. The predictive power of the QSAR was checked through the cross validation technique and also by leaving some compounds as part of external test set
Bangladesh Journal of Pharmacology, 2017
The methanolic extract of Alysicarpus vaginalis was selected for fractionation due to its known r... more The methanolic extract of Alysicarpus vaginalis was selected for fractionation due to its known reported biological activity. The four fractions were separated and subjected for in vitro antimitotic and anti-proliferative assays along with anti-cancer activity on two human cancers cell lines (SK-MEL-2 and Hep-G2). The antimicrobial potential of fractions had been evaluated against bacteria and fungi. From all fractions, acetone and n-butanol fractions were effective against the cell lines. They show strong inhibitory action with mitotic index 6.2 and 8.4 mg/mL and IC50 values of anti-proliferative assay in between 19.7 to 14.2 mg/mL respectively, which was found to be comparable to the standard methothrexate 5.9 mg/mL and 13.2 mg/mL respectively. In antimicrobial activity, the zone of inhibition had been observed in the range of 12-27 mm and MIC value was found in the range of 0.2-0.1 mg/mL. The acetone fraction was found to be most active against fungi, and E. coli whereas chlorofo...
Advanced Science Letters, 2016
Journal of Chemical & Engineering Data, 2015
Models for predicting the solubility of drugs in monosolvents and their mixtures have a practical... more Models for predicting the solubility of drugs in monosolvents and their mixtures have a practical importance in design and development of new products in pharmaceutical industries. Thus, present investigation pertains to the utility of a correlative model for solubility prediction of etoricoxib (ETR). The molar solubilities of ETR in a number of monosolvents and various mass fractions of their binary aqueous solvent mixtures were determined using the shakeflask method at 298.2 K. Densities of ETR saturated solutions in the monosolvents and their binary solvent mixtures were measured and then correlated using a well-established method proposed by Jouyban and Acree. Overall mean percentage deviations (OMPDs) between experimental and predicted values were 3.4 % for the molar solubilities and 0.1 % for the densities of the saturated solutions.
International Journal of Applied Pharmaceutics, 2015
Human body is known to experience positive stress that keeps it vigilant and protects it from bio... more Human body is known to experience positive stress that keeps it vigilant and protects it from biological and physical threats. This stress turns negative when a person is confronted with continuous challenges. Also, stress and nutrition have always run in synergism with each other. Nutritional value of a person's diet depends on the overall mixture or balance of food that is eaten over a period of time, as well as on the needs of the individual. The body relies on obtaining its anti-oxidants from food and other supplements. These nutritional requirements of antioxidants are enormously altered in diseased conditions. In view of the immense medicinal importance of antioxidants, an effort has been made in this article to bring together information about the role of nutrition and antioxidants such as carotenoids, vitamins, some important minerals in combating free radical generation and in general, boosting normal immune mechanisms. The present review is an attempt to generate interest in the scientific fraternity of their immense potential in preventing and treating several common diseases.
International Journal of Pharmacy and Pharmaceutical Sciences, 2014
There is a growing interest towards the development of new antibiotics from last decades due to e... more There is a growing interest towards the development of new antibiotics from last decades due to emergence of newer pathogenic bacterial strains with high resistance to powerful antibiotics of last resort. This has caused decline in research for developing newer antibacterial agents. Hence, there is continuous need to develop newer antibiotics that interact with essential mechanisms in bacteria. Recently, enzymes responsible for bio synthesis of the essential amino acid lysine in bacteria have been targeted and it has augmented interest to develop novel antibiotics and to enhance lysine yields in over-producing organisms. Peptidoglycan layer consists of a beta-1,4-linked polysaccharide of alternating N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAM) sugar units, cross linked by short pentapeptide (muramyl residues) side chain of general structure L-Ala-g-D-Glu-X-D-Ala-D-Ala, where X is either L-Lysine or meso-DAP. Formation of the cross-links makes bacterial cell wall resistant to lysis by intracellular osmotic pressure. Compounds which inhibit lysine or DAP biosynthesis could therefore be very effective antibiotics and novel targets. Lysine is a constituent in gram-positive bacteria while meso-DAP occurs in gram negative ones. In this review, substrate-based inhibitors of enzymes in the DAP pathway and inhibitors that allow better understanding of enzymology of the targets and provide insight for design of new inhibitors have been discussed. Resistant bacterial strains can be inhibited by using synthetic enzyme inhibitors of DAP pathway that are less toxic to mammals. Newer antimicrobial drugs can be thus developed by targeting the enzymes involved in this pathway.
Current Organic Synthesis, 2015
Substantial attention has been given in developing novel heterocyclic compounds as these have bee... more Substantial attention has been given in developing novel heterocyclic compounds as these have been found to exhibit varied biological activities. Benzothiazoles belong to one of the special categories of heterocyclic compounds with a wide range of biological activities such as antimicrobial, antitumor, antidiabetic, antitubercular, antimalarial, anticonvulsant, anthelmintic, analgesic, antiinflammatory and many more. These compounds have been serving as leads for researchers who are actively involved in synthesizing and evaluating their biological activities. Such an extensive work has stimulated further development of new benzothiazole derivatives with enhanced biological activities. This review focuses on the various approaches on the synthesis of benzothiazole derivatives viz., conventional, green, combinatorial and microwave-assisted methods. It also highlights various biological activities of the currently synthesized benzothiazoles.