Manjulatha Pujar | University of Hyderabad (original) (raw)
Papers by Manjulatha Pujar
Abstract- Worldwide, infectious disease is the number one cause of death accounting for approxima... more Abstract- Worldwide, infectious disease is the number one cause of death accounting for approximately one-half of all deaths in tropical countries. Resistant to conventional antibiotics is an important health concern and reason for the problem of multidrug resistance (MDR) resides on the fact that the current arsenal of antibiotics has been largely designed on limited chemical scaffolds with only few innovations leaving an opportunity for pathogens to develop and spread antibiotic resistance mechanisms worldwide. The complex molecules in nature have evolved over millennia to provide robust, disease-fighting mechanisms, intense biological activity as a result of natural selection. In present study Sapindus emarginatus fruits commonly known as soap berry, Ritta whose aqueous extract of pericarp is used as detergent that is evaluated for its antimicrobial potential and found to be have significant antimicrobial potential with lowest of 7.8 mg/ml against yeast Candida albicans, at 15.6 ...
Acalypha indica L (Family Euphorbiaceae) is used traditionally in Indian system of medicine for v... more Acalypha indica L (Family Euphorbiaceae) is used traditionally in Indian system of medicine for various ailments. Present study aims at the gastroprotective effect leaves and roots of Acalypha indica which were administered orally as pre-treatment for Aspirin (ASP), cold-restraint stress (CRS), pylorus ligation (PLU) and ethanol (EIU), induced ulcers. Estimation of gastric secretion parameters like volume of gastric juice, acid output, and pH value were estimated in PLU and EIU induced ulcer model. The results of the study revealed that Acalypha indica roots ethanolic extract showed dosedependent ulcer protective effect on peptic ulcers induced by physical and chemical agents in rodents.
Molecular Crystals and Liquid Crystals
Novel aurone derivatives e.g. 2-(2-(3-methylbut-2-enyloxy)benzylidene)benzofuran-3(2H)-one (3a), ... more Novel aurone derivatives e.g. 2-(2-(3-methylbut-2-enyloxy)benzylidene)benzofuran-3(2H)-one (3a), 2-(2-(allyloxy)benzylidene)-7-methoxybenzofuran-3(2H)-one (3b), and 2-(5-bromo-2-(3-methylbut-2-enyloxy)benzylidene)-6-hydroxybenzofuran-3(2H)-one (3c) were synthesized. All these compounds were characterized by IR, 1H and 13C NMR, and Mass spectroscopy. Finally, the crystal structures were solved by single crystal X-ray diffraction data and the structures were analyzed in terms of supramolecular interactions.[Supplementary materials are available for this article. Go to the publisher's online edition of Molecular Crystals and Liquid Crystals for the following free supplemental resource(s): supplemental figures 1–12; Spectral data (IR, NMR, MS, and HRMS) of the compounds 3a, 3b and 3c are available in the supporting information in .pdf format. Crystallographic information files (.cif) of compounds 3a, 3b, and 3c are available in the electronic format.]
Hemidesmus indicus (L.) R. Br. has been revered for its medicinal properties for nearly a thousan... more Hemidesmus indicus (L.) R. Br. has been revered for its medicinal properties for nearly a thousand years in Indian traditional medicine, Ayurveda and commonly known as Indian Sarsaparilla/Anantamool/Sariva. It is used as a vital herb for healing many ailments and considered as magical spiritual dream herb in Ayurvedic medication. It has long been used in Indian folk medicine to treat diversified diseases such as liver diseases, asthma, arthritis, bronchitis, syphilis, epileptic seizures, high blood pressure, skin diseases (eczema and psoriasis), rheumatism, chronic nervous diseases, impotence and immune disorders. Mainly the roots of this plant are endowed with many pharmacological properties and since long enjoyed a reputation as tonic, alterative, diaphoretic, diuretic, depurative. It is also known to help relieving stress by inducing overwhelming sensation of relaxation, euphoria and tranquility. It forms an important ingredient in “Sarivadyasava” an Ayurvedic preparation used in...
Ethnopharmacological relevance: Albizzia lebbeck Benth is a medicinal plant traditionally used to... more Ethnopharmacological relevance: Albizzia lebbeck Benth is a medicinal plant traditionally used to treat various ailments, including ulcers In order to establish pharmacological properties of the bark of Albizzia lebbeck, studies were performed on antiulcer activity of the plant’s methanolic extract. The Albizzia lebbeck methanolic extract (ALME) was prepared in the doses of 100, 200 mg/kg. Antiulcer activity of ALME was evaluated by aspirin induced gastric ulcer. Acute toxicity was also carried out. ALME, at the dose of 5000 mg/kg, did not cause any signs of toxicity to rats when given orally. Oral administration of ALME exhibited antiulcer activity. Histological studies supported the observed antiulcer activity of ALME. The ALME exhibits antiulcer activity, which could be due to the presence of flavonoids of Albizzia lebbeck in the treatment of ulcers.
Albizzia lebbeck Benth (Family Mimoseaceae) is used traditionally in Indian System of Medicine fo... more Albizzia lebbeck Benth (Family Mimoseaceae) is used traditionally in Indian System of Medicine for various ailments. Present study aims at the gastroprotective effect ethylacetate and saponin fraction of Albizzia lebbeck bark which were administered orally as pretreatment for ethanol (EtOH), cold-restraint stress (CRS) and pylorus ligation (PL) induced ulcers. Estimation of gastric secretion parameters like volume of gastric juice, acid output, and pH value were estimated in PL induced ulcer model. The results of our study revealed that Albizzia lebbeck bark ethylacetate extract showed dose-dependent ulcer protective effect on peptic ulcers induced by physical and chemical agents in rodents.
[
Indian Journal of Heterocyclic Chemistry
The esterification of 1-alkyl/aryl-3-ethoxy carbonyl-5-hydroxy-2-methyl indoles (1a-g) with ethyl... more The esterification of 1-alkyl/aryl-3-ethoxy carbonyl-5-hydroxy-2-methyl indoles (1a-g) with ethyl chloroacetate and ethyl chloroformate, afforded ethyl 5-(ethoxycarbonyl) methoxy]-1alkyl/aryl-2-methyl-indole-3-carboxylate (2a-g) and 3-(ethoxycarbonyl)-1-alkyl/aryl-2-methyl-1H-indol-5-yl ethyl carbonate (3a-g) respectively. The reaction of 1b-g with monochloroacetic acid and 2-chloropropionic acid afforded the corresponding indole acetic acid (4b-g) and propanoic acid (5b-g) derivatives respectively. These newly synthesized compounds were evaluated in vivo for potential anti-inflammatory and analgesic activities and the results were compared with indomethacin. These analogues were administered p.o. at a dose level of 20 mg/kg.
In the present study Dodonaea viscosa plant secondary metabolites were extracted using various so... more In the present study Dodonaea viscosa plant secondary metabolites were extracted using various solvents from whole plant, its roots, aerial part, stem, leaves, and seeds were investigated for phenolics and flavonoids content, antimicrobial and antioxidant property. The phenolics and flavonoids contents were determined by spectrophotometric method. The antimicrobial activities were assessed by measuring the diameter of the inhibition zones and minimum inhibition concentration values. The antioxidant activity is carried out by 2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH) assay which is common, fast and reliable to assess free radical scavenging ability of present study plant extracts. Present comparative study the data reveals that the concentration levels of phenolics and flavonoids vary in different parts of the plant in their various solvent extracts. In the investigation it was observed that phenolics and flavonoids were in higher concentration in ethylacetate and methanolic extra...
Abstract: This study is aimed to determine the in vitro antimicrobial activity of plant extracts ... more Abstract: This study is aimed to determine the in vitro antimicrobial activity of plant extracts from Gulbarga region of Karnataka, India against dermatophytes, yeast and bacteria. Fifteen plants were selected on the basis of literature survey of traditional and folk medicine for microbial infections. The plants were collected and extracted each separately with 95% ethanol under cold conditions. The phytochemicals were qualitatively and quantitatively determined. By agar dilution method the MIC values were obtained of ethanolic extracts derived from the 15 plants that exhibited anti-microbial activity ranging between 2-0.25 mg/ml. MIC values for the Aloe vera, Boerhaavia diffusa and Lawsonia inermis found to be active against Streptococccus pyogens and Staphylococcus aureus with MIC of 0.25 mg/ml. Among above three except Aloe vera was not active against Staphylococcus aureus at 0.5 mg/ml. Key words: antimicrobial activity, dermatophytes, bacteria, yeast, medicinal plants
ChemInform
A series of fused thiazolo[3,2-a] pyrimidines (7a=g, 8a=f, 11a=g and 12a, b) have been synthesize... more A series of fused thiazolo[3,2-a] pyrimidines (7a=g, 8a=f, 11a=g and 12a, b) have been synthesized in good yields by reaction of fused 3,4-dihydropyrimidin-2(1H)-thiones(4a-g) with phenacyl bromides ( 5,6)/3-(2- bromoacetyl) coumarins (9,10) under conventional heating in acetic acid. Analytical and spectral studies as well as single crystal X-ray diffraction data on the representative compound 8e confirmed the structure of all the reaction products. All the synthesized compounds were screened for their antibacterial, antioxidant and DNA cleavage activities. The compound 7e against Escherichia coli, 8a and 8c-e against Pseudomonas aeruginosa have shown prominent antibacterial activity compared to the standard drug Penicillin with MIC 9.375 mu g mL(-1), whereas the compounds 11c, 12a and 12b have shown very good antioxidant activity compared to the standard drug Trolox with IC50 values 12.36, 11.12 and 13.88 mu M respectively. Compounds 11f and 12b have completely cleaved the DNA even...
Frontiers in Microbiology, 2015
Herbal products derived from Hemidesmus indicus (L.) R. Br. ex Schult, Leucas aspera (Wild.), Plu... more Herbal products derived from Hemidesmus indicus (L.) R. Br. ex Schult, Leucas aspera (Wild.), Plumbago zeylanica L., and Tridax procumbens (L.) R. Br. ex Schult. are widely used in traditional medicine. Though the extracts of these plants were found to be antimicrobial in nature and have the potential to be used in clinics, the mechanism of action of is not reported. The ethanolic extracts of Hemidesmus indicus (L.) R. Br. ex Schult, Hemidesmus indicus ethanolic extract (HIEE), Leucas aspera (Wild.), Leucas aspera ethanolic extract (LAEE), Plumbago zeylanica L., Plumbago zeylanica ethanolic extract (PZEE), and Tridax procumbens (L.) R. Br. ex Schult, Tridax procumbens ethanolic extract (TPEE) were tested for their antibacterial activity against E. coli. Antibacterial activity was analyzed by CFU assay and the effect on the bacterial membrane by fluorescence activated cell sorting and scanning electron microscopy. LAEE, PZEE, and HIEE displayed potent bacterial killing activity in a time and concentration dependent manner. TPEE did not display appreciable antibacterial activity. The antibacterial action involved disruption of membrane potential, inner membrane permeabilization, blebbing and leakage of cellular contents. Our results contribute to the understanding of the antibacterial mechanism of alcoholic extracts of the medicinal plants used in this study.
Medicinal Chemistry Research, 2015
ABSTRACT Chrysin and 7-hydroxy flavone were prepared by Baker–Venkatraman rearrangement followed ... more ABSTRACT Chrysin and 7-hydroxy flavone were prepared by Baker–Venkatraman rearrangement followed by esterification at 7th position and replacement of ester with acetamide linking to different heterocyclic moieties synthesized 13a–g and 14a–g series of flavones analogues. These were screened against COX-2 and COX-1 enzymes for inhibition by in vitro assay and COX-2 for in silico docking studies. The compound 14a was found to be most active with IC50 of 3.11 µM concentration, with highest binding energy of −12.4 kcal/mole and 77.2 and 80.5 % inhibition at 3 and 5 h post-carrageenan induced in paw oedema.
Vedic Research International Phytomedicine, 2013
BioMed Research International, 2014
Nyctanthes arbortristisL. (Oleaceae) is widely used in the Indian system of traditional medicine ... more Nyctanthes arbortristisL. (Oleaceae) is widely used in the Indian system of traditional medicine and is reported to have various biological activities. The present study was intended to evaluate the antioxidant and antiproliferative activities of flower extracts ofNyctanthes arbortristis. The shade dried flowers were extracted with 95% ethanol under sonication and the antioxidant activities were investigated usingin vitroassays along with the determination of phytochemical constituents (total polyphenol and total flavonoid). Arborside C andβ-monogentiobioside ester ofα-Crocetin were identified in crude active extracts through LCMS/MS analysis. The antiproliferative activity was carried out by MTT assay by employing different human cancer cell lines. The lowest IC50value of 24.56 ± 6.63 μg/mL was observed against Colo 205 cell line. The extract exhibited significant antioxidant and antiproliferative properties and the observed biological activities in this study provide scientific va...
Bioorganic & Medicinal Chemistry Letters, 2012
An improved synthesis of functionalized aurones has been accomplished via the reaction of benzofu... more An improved synthesis of functionalized aurones has been accomplished via the reaction of benzofuran-3(2H)-one with a range of benzaldehydes in the presence of a mild base EDDA under ultrasound. A number of aurones were synthesized (within 5-30min) and the molecular structure of a representative compound determined by single crystal X-ray diffraction study confirmed Z-geometry of the C-C double bond present within the molecule. Some of the compounds synthesized have shown SIRT1 inhibiting as well as anti proliferative properties against two cancer cell lines in vitro. Compound 3a [(Z)-2-(5-bromo-2-hydroxybenzylidene) benzofuran-3(2H)-one] was identified as a potent inhibitor of SIRT1 (IC(50)=1μM) which showed a dose dependent increase in the acetylation of p53 resulting in induction of apoptosis.
Bioorganic & medicinal …, 2010
Tetrahedron Letters, 2010
A novel one-pot eco-friendly protocol for the synthesis of 2-benzazepine derivatives in water has... more A novel one-pot eco-friendly protocol for the synthesis of 2-benzazepine derivatives in water has been developed. 4-Chloro-3-formyl coumarin reacts with benzyl amines under catalyst-free conditions in aqueous medium to afford substituted 5-(2 0-hydroxyaryl)-4-amido-2-benzazepines in excellent yields.
Bioorganic & medicinal …, 2006
Two new furanoflavonoids (1, 2), one new chalcone dimer (3) along with six known compounds, chrys... more Two new furanoflavonoids (1, 2), one new chalcone dimer (3) along with six known compounds, chrysophanol, 5-O-methyl squarrosin, 5-methoxy furano[4″,5″,6,7]flavone, calodenone, lophirone A and lophirone H were isolated from the ethyl acetate-soluble ...
Synlett, 2010
Diels-Alder reaction of furan with electron-deficient 3carbethoxycoumarins gave the Michael-type ... more Diels-Alder reaction of furan with electron-deficient 3carbethoxycoumarins gave the Michael-type adducts obtained from the rearrangement of the intermediate Diels-Alder adducts, instead of the Diels-Alder cycloadducts. Trapping of the dipolar intermediate with electron-deficient aromatic aldehydes gave a one-pot access to fused furo[3,2-b]pyranochroman-2-ones with multiple stereogenic centers. Ring opening of the lactone moiety gave a facile route to generate diverse scaffolds.
Journal of Saudi Chemical Society, 2011
A new series of 6-iodo-2-phenylquinazolin-4(3H)-one derivatives was prepared and screened for ant... more A new series of 6-iodo-2-phenylquinazolin-4(3H)-one derivatives was prepared and screened for antimicrobial activity. The thioureide derivatives 4–6, the carbohydrazide derivatives 19–21 and 24 displayed excellent broad-spectrum antimicrobial activity. Some compounds showed moderate activity against Candida albicans and Pseudomonas aeruginosa. None of the tested compounds was as active as the reference standard drugs ampicillin and clotrimazole. The detailed synthesis, antimicrobial activity,
Abstract- Worldwide, infectious disease is the number one cause of death accounting for approxima... more Abstract- Worldwide, infectious disease is the number one cause of death accounting for approximately one-half of all deaths in tropical countries. Resistant to conventional antibiotics is an important health concern and reason for the problem of multidrug resistance (MDR) resides on the fact that the current arsenal of antibiotics has been largely designed on limited chemical scaffolds with only few innovations leaving an opportunity for pathogens to develop and spread antibiotic resistance mechanisms worldwide. The complex molecules in nature have evolved over millennia to provide robust, disease-fighting mechanisms, intense biological activity as a result of natural selection. In present study Sapindus emarginatus fruits commonly known as soap berry, Ritta whose aqueous extract of pericarp is used as detergent that is evaluated for its antimicrobial potential and found to be have significant antimicrobial potential with lowest of 7.8 mg/ml against yeast Candida albicans, at 15.6 ...
Acalypha indica L (Family Euphorbiaceae) is used traditionally in Indian system of medicine for v... more Acalypha indica L (Family Euphorbiaceae) is used traditionally in Indian system of medicine for various ailments. Present study aims at the gastroprotective effect leaves and roots of Acalypha indica which were administered orally as pre-treatment for Aspirin (ASP), cold-restraint stress (CRS), pylorus ligation (PLU) and ethanol (EIU), induced ulcers. Estimation of gastric secretion parameters like volume of gastric juice, acid output, and pH value were estimated in PLU and EIU induced ulcer model. The results of the study revealed that Acalypha indica roots ethanolic extract showed dosedependent ulcer protective effect on peptic ulcers induced by physical and chemical agents in rodents.
Molecular Crystals and Liquid Crystals
Novel aurone derivatives e.g. 2-(2-(3-methylbut-2-enyloxy)benzylidene)benzofuran-3(2H)-one (3a), ... more Novel aurone derivatives e.g. 2-(2-(3-methylbut-2-enyloxy)benzylidene)benzofuran-3(2H)-one (3a), 2-(2-(allyloxy)benzylidene)-7-methoxybenzofuran-3(2H)-one (3b), and 2-(5-bromo-2-(3-methylbut-2-enyloxy)benzylidene)-6-hydroxybenzofuran-3(2H)-one (3c) were synthesized. All these compounds were characterized by IR, 1H and 13C NMR, and Mass spectroscopy. Finally, the crystal structures were solved by single crystal X-ray diffraction data and the structures were analyzed in terms of supramolecular interactions.[Supplementary materials are available for this article. Go to the publisher's online edition of Molecular Crystals and Liquid Crystals for the following free supplemental resource(s): supplemental figures 1–12; Spectral data (IR, NMR, MS, and HRMS) of the compounds 3a, 3b and 3c are available in the supporting information in .pdf format. Crystallographic information files (.cif) of compounds 3a, 3b, and 3c are available in the electronic format.]
Hemidesmus indicus (L.) R. Br. has been revered for its medicinal properties for nearly a thousan... more Hemidesmus indicus (L.) R. Br. has been revered for its medicinal properties for nearly a thousand years in Indian traditional medicine, Ayurveda and commonly known as Indian Sarsaparilla/Anantamool/Sariva. It is used as a vital herb for healing many ailments and considered as magical spiritual dream herb in Ayurvedic medication. It has long been used in Indian folk medicine to treat diversified diseases such as liver diseases, asthma, arthritis, bronchitis, syphilis, epileptic seizures, high blood pressure, skin diseases (eczema and psoriasis), rheumatism, chronic nervous diseases, impotence and immune disorders. Mainly the roots of this plant are endowed with many pharmacological properties and since long enjoyed a reputation as tonic, alterative, diaphoretic, diuretic, depurative. It is also known to help relieving stress by inducing overwhelming sensation of relaxation, euphoria and tranquility. It forms an important ingredient in “Sarivadyasava” an Ayurvedic preparation used in...
Ethnopharmacological relevance: Albizzia lebbeck Benth is a medicinal plant traditionally used to... more Ethnopharmacological relevance: Albizzia lebbeck Benth is a medicinal plant traditionally used to treat various ailments, including ulcers In order to establish pharmacological properties of the bark of Albizzia lebbeck, studies were performed on antiulcer activity of the plant’s methanolic extract. The Albizzia lebbeck methanolic extract (ALME) was prepared in the doses of 100, 200 mg/kg. Antiulcer activity of ALME was evaluated by aspirin induced gastric ulcer. Acute toxicity was also carried out. ALME, at the dose of 5000 mg/kg, did not cause any signs of toxicity to rats when given orally. Oral administration of ALME exhibited antiulcer activity. Histological studies supported the observed antiulcer activity of ALME. The ALME exhibits antiulcer activity, which could be due to the presence of flavonoids of Albizzia lebbeck in the treatment of ulcers.
Albizzia lebbeck Benth (Family Mimoseaceae) is used traditionally in Indian System of Medicine fo... more Albizzia lebbeck Benth (Family Mimoseaceae) is used traditionally in Indian System of Medicine for various ailments. Present study aims at the gastroprotective effect ethylacetate and saponin fraction of Albizzia lebbeck bark which were administered orally as pretreatment for ethanol (EtOH), cold-restraint stress (CRS) and pylorus ligation (PL) induced ulcers. Estimation of gastric secretion parameters like volume of gastric juice, acid output, and pH value were estimated in PL induced ulcer model. The results of our study revealed that Albizzia lebbeck bark ethylacetate extract showed dose-dependent ulcer protective effect on peptic ulcers induced by physical and chemical agents in rodents.
[
Indian Journal of Heterocyclic Chemistry
The esterification of 1-alkyl/aryl-3-ethoxy carbonyl-5-hydroxy-2-methyl indoles (1a-g) with ethyl... more The esterification of 1-alkyl/aryl-3-ethoxy carbonyl-5-hydroxy-2-methyl indoles (1a-g) with ethyl chloroacetate and ethyl chloroformate, afforded ethyl 5-(ethoxycarbonyl) methoxy]-1alkyl/aryl-2-methyl-indole-3-carboxylate (2a-g) and 3-(ethoxycarbonyl)-1-alkyl/aryl-2-methyl-1H-indol-5-yl ethyl carbonate (3a-g) respectively. The reaction of 1b-g with monochloroacetic acid and 2-chloropropionic acid afforded the corresponding indole acetic acid (4b-g) and propanoic acid (5b-g) derivatives respectively. These newly synthesized compounds were evaluated in vivo for potential anti-inflammatory and analgesic activities and the results were compared with indomethacin. These analogues were administered p.o. at a dose level of 20 mg/kg.
In the present study Dodonaea viscosa plant secondary metabolites were extracted using various so... more In the present study Dodonaea viscosa plant secondary metabolites were extracted using various solvents from whole plant, its roots, aerial part, stem, leaves, and seeds were investigated for phenolics and flavonoids content, antimicrobial and antioxidant property. The phenolics and flavonoids contents were determined by spectrophotometric method. The antimicrobial activities were assessed by measuring the diameter of the inhibition zones and minimum inhibition concentration values. The antioxidant activity is carried out by 2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH) assay which is common, fast and reliable to assess free radical scavenging ability of present study plant extracts. Present comparative study the data reveals that the concentration levels of phenolics and flavonoids vary in different parts of the plant in their various solvent extracts. In the investigation it was observed that phenolics and flavonoids were in higher concentration in ethylacetate and methanolic extra...
Abstract: This study is aimed to determine the in vitro antimicrobial activity of plant extracts ... more Abstract: This study is aimed to determine the in vitro antimicrobial activity of plant extracts from Gulbarga region of Karnataka, India against dermatophytes, yeast and bacteria. Fifteen plants were selected on the basis of literature survey of traditional and folk medicine for microbial infections. The plants were collected and extracted each separately with 95% ethanol under cold conditions. The phytochemicals were qualitatively and quantitatively determined. By agar dilution method the MIC values were obtained of ethanolic extracts derived from the 15 plants that exhibited anti-microbial activity ranging between 2-0.25 mg/ml. MIC values for the Aloe vera, Boerhaavia diffusa and Lawsonia inermis found to be active against Streptococccus pyogens and Staphylococcus aureus with MIC of 0.25 mg/ml. Among above three except Aloe vera was not active against Staphylococcus aureus at 0.5 mg/ml. Key words: antimicrobial activity, dermatophytes, bacteria, yeast, medicinal plants
ChemInform
A series of fused thiazolo[3,2-a] pyrimidines (7a=g, 8a=f, 11a=g and 12a, b) have been synthesize... more A series of fused thiazolo[3,2-a] pyrimidines (7a=g, 8a=f, 11a=g and 12a, b) have been synthesized in good yields by reaction of fused 3,4-dihydropyrimidin-2(1H)-thiones(4a-g) with phenacyl bromides ( 5,6)/3-(2- bromoacetyl) coumarins (9,10) under conventional heating in acetic acid. Analytical and spectral studies as well as single crystal X-ray diffraction data on the representative compound 8e confirmed the structure of all the reaction products. All the synthesized compounds were screened for their antibacterial, antioxidant and DNA cleavage activities. The compound 7e against Escherichia coli, 8a and 8c-e against Pseudomonas aeruginosa have shown prominent antibacterial activity compared to the standard drug Penicillin with MIC 9.375 mu g mL(-1), whereas the compounds 11c, 12a and 12b have shown very good antioxidant activity compared to the standard drug Trolox with IC50 values 12.36, 11.12 and 13.88 mu M respectively. Compounds 11f and 12b have completely cleaved the DNA even...
Frontiers in Microbiology, 2015
Herbal products derived from Hemidesmus indicus (L.) R. Br. ex Schult, Leucas aspera (Wild.), Plu... more Herbal products derived from Hemidesmus indicus (L.) R. Br. ex Schult, Leucas aspera (Wild.), Plumbago zeylanica L., and Tridax procumbens (L.) R. Br. ex Schult. are widely used in traditional medicine. Though the extracts of these plants were found to be antimicrobial in nature and have the potential to be used in clinics, the mechanism of action of is not reported. The ethanolic extracts of Hemidesmus indicus (L.) R. Br. ex Schult, Hemidesmus indicus ethanolic extract (HIEE), Leucas aspera (Wild.), Leucas aspera ethanolic extract (LAEE), Plumbago zeylanica L., Plumbago zeylanica ethanolic extract (PZEE), and Tridax procumbens (L.) R. Br. ex Schult, Tridax procumbens ethanolic extract (TPEE) were tested for their antibacterial activity against E. coli. Antibacterial activity was analyzed by CFU assay and the effect on the bacterial membrane by fluorescence activated cell sorting and scanning electron microscopy. LAEE, PZEE, and HIEE displayed potent bacterial killing activity in a time and concentration dependent manner. TPEE did not display appreciable antibacterial activity. The antibacterial action involved disruption of membrane potential, inner membrane permeabilization, blebbing and leakage of cellular contents. Our results contribute to the understanding of the antibacterial mechanism of alcoholic extracts of the medicinal plants used in this study.
Medicinal Chemistry Research, 2015
ABSTRACT Chrysin and 7-hydroxy flavone were prepared by Baker–Venkatraman rearrangement followed ... more ABSTRACT Chrysin and 7-hydroxy flavone were prepared by Baker–Venkatraman rearrangement followed by esterification at 7th position and replacement of ester with acetamide linking to different heterocyclic moieties synthesized 13a–g and 14a–g series of flavones analogues. These were screened against COX-2 and COX-1 enzymes for inhibition by in vitro assay and COX-2 for in silico docking studies. The compound 14a was found to be most active with IC50 of 3.11 µM concentration, with highest binding energy of −12.4 kcal/mole and 77.2 and 80.5 % inhibition at 3 and 5 h post-carrageenan induced in paw oedema.
Vedic Research International Phytomedicine, 2013
BioMed Research International, 2014
Nyctanthes arbortristisL. (Oleaceae) is widely used in the Indian system of traditional medicine ... more Nyctanthes arbortristisL. (Oleaceae) is widely used in the Indian system of traditional medicine and is reported to have various biological activities. The present study was intended to evaluate the antioxidant and antiproliferative activities of flower extracts ofNyctanthes arbortristis. The shade dried flowers were extracted with 95% ethanol under sonication and the antioxidant activities were investigated usingin vitroassays along with the determination of phytochemical constituents (total polyphenol and total flavonoid). Arborside C andβ-monogentiobioside ester ofα-Crocetin were identified in crude active extracts through LCMS/MS analysis. The antiproliferative activity was carried out by MTT assay by employing different human cancer cell lines. The lowest IC50value of 24.56 ± 6.63 μg/mL was observed against Colo 205 cell line. The extract exhibited significant antioxidant and antiproliferative properties and the observed biological activities in this study provide scientific va...
Bioorganic & Medicinal Chemistry Letters, 2012
An improved synthesis of functionalized aurones has been accomplished via the reaction of benzofu... more An improved synthesis of functionalized aurones has been accomplished via the reaction of benzofuran-3(2H)-one with a range of benzaldehydes in the presence of a mild base EDDA under ultrasound. A number of aurones were synthesized (within 5-30min) and the molecular structure of a representative compound determined by single crystal X-ray diffraction study confirmed Z-geometry of the C-C double bond present within the molecule. Some of the compounds synthesized have shown SIRT1 inhibiting as well as anti proliferative properties against two cancer cell lines in vitro. Compound 3a [(Z)-2-(5-bromo-2-hydroxybenzylidene) benzofuran-3(2H)-one] was identified as a potent inhibitor of SIRT1 (IC(50)=1μM) which showed a dose dependent increase in the acetylation of p53 resulting in induction of apoptosis.
Bioorganic & medicinal …, 2010
Tetrahedron Letters, 2010
A novel one-pot eco-friendly protocol for the synthesis of 2-benzazepine derivatives in water has... more A novel one-pot eco-friendly protocol for the synthesis of 2-benzazepine derivatives in water has been developed. 4-Chloro-3-formyl coumarin reacts with benzyl amines under catalyst-free conditions in aqueous medium to afford substituted 5-(2 0-hydroxyaryl)-4-amido-2-benzazepines in excellent yields.
Bioorganic & medicinal …, 2006
Two new furanoflavonoids (1, 2), one new chalcone dimer (3) along with six known compounds, chrys... more Two new furanoflavonoids (1, 2), one new chalcone dimer (3) along with six known compounds, chrysophanol, 5-O-methyl squarrosin, 5-methoxy furano[4″,5″,6,7]flavone, calodenone, lophirone A and lophirone H were isolated from the ethyl acetate-soluble ...
Synlett, 2010
Diels-Alder reaction of furan with electron-deficient 3carbethoxycoumarins gave the Michael-type ... more Diels-Alder reaction of furan with electron-deficient 3carbethoxycoumarins gave the Michael-type adducts obtained from the rearrangement of the intermediate Diels-Alder adducts, instead of the Diels-Alder cycloadducts. Trapping of the dipolar intermediate with electron-deficient aromatic aldehydes gave a one-pot access to fused furo[3,2-b]pyranochroman-2-ones with multiple stereogenic centers. Ring opening of the lactone moiety gave a facile route to generate diverse scaffolds.
Journal of Saudi Chemical Society, 2011
A new series of 6-iodo-2-phenylquinazolin-4(3H)-one derivatives was prepared and screened for ant... more A new series of 6-iodo-2-phenylquinazolin-4(3H)-one derivatives was prepared and screened for antimicrobial activity. The thioureide derivatives 4–6, the carbohydrazide derivatives 19–21 and 24 displayed excellent broad-spectrum antimicrobial activity. Some compounds showed moderate activity against Candida albicans and Pseudomonas aeruginosa. None of the tested compounds was as active as the reference standard drugs ampicillin and clotrimazole. The detailed synthesis, antimicrobial activity,