Background: 5α-Reductase (5AR), an NADPH dependent enzyme, is expressed in most of the prostate e... more Background: 5α-Reductase (5AR), an NADPH dependent enzyme, is expressed in most of the prostate epithelial cells. By converting testosterone (T) into more potent androgen dihydrotestosterone (DHT), it plays an important role in men physiology and represents an efficient therapeutic target for androgen-dependent diseases. Over the last few years, significant efforts have been made in order to develop 5AR inhibitors (5ARI) to treat Benign Prostatic Hyperplasia because of excessive production of DHT. Methods: In the present study, 2D and 3D QSAR pharmacophore models have been generated for 5ARI based on known IC50 values with extensive validations. The four featured 2D pharmacophore based PLS model correlated the topological interactions (SsOHE-index); semi empirical (Quadrupole2) and physicochemical descriptors (Mol. Wt, Bromines Count, Chlorines Count) with 5AR inhibitory activity, and has the highest correlation coefficient (r2 = 0.98, q2 =0.84; F = 57.87, pred r2 = 0.88). Internal ...
Convolvulus arvensis is a long lived deep rooted weed belongs to the family Convolvulaceae. It is... more Convolvulus arvensis is a long lived deep rooted weed belongs to the family Convolvulaceae. It is commonly known as European bindweed, bindweed, creeping jenny, morning glory, and devil’s guts. It has at least 84 common names. Field bindweed is found in a wide range of habitats: orchards, vineyards, roadsides, ditch banks, cropland, steam banks, and lakeshores. Field bindweed begins growing in the late spring or early summer and may persist until the first frost. It is most likely confused with the Ipomoea spp., Calystegia spp., Dioscorea spp, Polygonum convolvulus L. It is very much difficult to differentiate between all these species. The plant contains Saponins, Alkaloids, and Polyphenolic compounds Flavonoids and Tannins. It has stimulant, anti-oxidant, anticancer and laxative effect. This review shows its identification, some of the isolated compounds and its biological activities.
Steroids have contributed a lot in the development of organic chemistry. The broad operations of ... more Steroids have contributed a lot in the development of organic chemistry. The broad operations of biological activity and multiplicity of action make steroids one of the most intriguing classes of biologically active compounds. The area has been very fascinating for the study of reaction mechanisms and stereochemistry and a brief discussion on neuromuscular blocking agents is discussed below.
Chronic myelogenous leukaemia is one of the major chronic myeloproliferative diseases of pluipote... more Chronic myelogenous leukaemia is one of the major chronic myeloproliferative diseases of pluipotential haematopoietic stem cells. Many therapeautic agents have failed to provide any relief to the patients suffering from chronic myelogenous leukaemia (CML). Imatinib was first ever developed drug for the treatment of (CML) but the problem associated with it is the resistant against this drug. Therefore, the development of new agents will remain an important challenging task for medicinal chemists. So, there is an urgent need for identification of new, potent, and less toxic agents which ideally shorten the duration of therapy and are effective against CML. Nilotinib which are found to be effective in patient with Imatinib – resistant chronic myelogenous leukaemia (CML). It is a second generation BCR-ABL tyrosine kinase inhibitor and found to be target specific kinase inhibitor as compare with Imatinib. This reviews article reflects development of Nolotinib, mechanism of action, precli...
From the recent studies, 3,5-dibenzoyl-1,4-dihydropyridone (DHP) derivatives, DP-7, has emerged a... more From the recent studies, 3,5-dibenzoyl-1,4-dihydropyridone (DHP) derivatives, DP-7, has emerged as a potent multidrug reverting agent that inhibits efflux of drug from cell wall by inhibiting the activity of ATP Binding Cassettes. On the other hand, dihydropyrimidine (DHPM) derivative, (aza analogue) namely, monastrol inhibits the protein Eg5, which is responsible for the separation of daughter chromosomes during cell division and controls the growth of the tumor cells. In the present report, we have reported the hybridize molecules of these two potent molecules to check the dual action in cancer chemotherapy by synthesizing various thio and oxo analogues, bearing substituted aryl groups at 4th position of the DHPM ring. The newly synthesized molecules were screened for antiproliferative effects in mdr1-gene transfected mouse lymphoma cell line (l5178 y). Among these newly synthesized compounds namely, II h, I g, I i, and I j showed a very potent antiproliferative activity.
17-aza steroids are the important class of compounds used as 5α-reductase inhibitors for the trea... more 17-aza steroids are the important class of compounds used as 5α-reductase inhibitors for the treatment of benign prostatichyperplasia. As these agents blocks the conversion of Testosterone (T) into Dihydrotestosterone (DHT) which is the mainreason for the development of benign prostatic hyperplasia. Benign prostatic hyperplasia (BPH) is the noncancerousproliferation of the prostate gland associated with benign prostatic obstruction and lower urinary tract symptoms (LUTS)such as frequency, hesitancy and urgency. Its prevalence increases with age affecting around 70% by the age of 70 years.Main attention given to the 17-aza steroids is due to the back binding or inverted action that was proposed by Mac Donald et al. In this review, different 17-aza steroids such as seco-steroids, alkyl chain derivates at 17-position, 3β-esters and many other derivatives were shown.
International Journal of Pharmacognosy and Phytochemical Research
We herein report the synthesis of 3β-substituted amides of 17a-aza-D-homo-4-androsten-17-one (11a... more We herein report the synthesis of 3β-substituted amides of 17a-aza-D-homo-4-androsten-17-one (11a-11r) from commercially available Diosgenin as the starting material. The structures of newly synthesized compounds were confirmed by IR, (1)H NMR, (13)C NMR and mass spectrometry. All the synthesized analogues were tested for their 5α- reductase inhibitory and antimicrobial activity, some of them exhibit moderate to potent activity comparable to the reference drugs. Among the synthesized derivatives the analogue (11r) 3β-(indonlylbutanamido)-17a-aza-D-homo-4- androsten-17-one was found to be active against both 5α-reductase enzyme and microbial strains, whereas the analogue (11i) 3β-(3,4-dimethoxy-benzamido)-17a-aza-D-homo-4-androsten-17-one was found to be the least active. The detailed 5α-reductase inhibitors and antimicrobial activities of the synthesized compounds were reported.
In the present study, (E)-2-{ [-2-(2,4-Dinitrophenyl)hydrazono]methyl} phenol (3) was synthesized... more In the present study, (E)-2-{ [-2-(2,4-Dinitrophenyl)hydrazono]methyl} phenol (3) was synthesized and used as key intermediate for the synthesis of new Mannich bases. All the synthesized compounds were evaluated for their antifungal activity against three fungal strains Candida albicans, Candida tropicalis and Aspergillus niger and antioxidant activity. The structure of these compounds was confirmed by IR, 1H NMR and 13C NMR studies. Most of the compounds exhibited moderate to significant activities.
A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by ... more A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by coupling it with different substituted aldehydes, acetophenone, and benzophenones in presence of absolute ethanol along with catalytic amount of glacial acetic acid. All the synthesized compound were confirmed and characterized by using various spectral technique like IR, 1H NMR, 13C NMR, and mass spectroscopy studies. Anticonvulsant evaluations of all the synthesized compounds were done using various seizures models like maximal electroshock-induced seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) at a dose of 30, 100, and 300 mg/kg body weight and anticonvulsant activity was noted at 0.5 h and 4 h time intervals after the drug administration. Compound 1a (E)-N′-2-benzylidene isonicotinohydrazide, 1g (E)-N′-2-ethoxybenzylidene isonicotinohydrazide, 1k (E)-N′-3-flourobenzylidene isonicotinohydrazide and 3a (E)-N′-diphenylmethylene isonicotinohydrazide showed protection in MES mo...
In the present study, a series of (Z)-N-(1-[2-{3-[(dimethylamino)methyl)]-2-methoxyphenyl}-5-(pyr... more In the present study, a series of (Z)-N-(1-[2-{3-[(dimethylamino)methyl)]-2-methoxyphenyl}-5-(pyridin-4-yl)-1,3,4-oxadiazol-3(2H)-yl]ethylidene)benzenamine derivatives have been synthesized and characterized by IR, 1H NMR and 13C NMR spectra. All the synthesized compounds were evaluated for their antifungal activity and were compared with the standard drug, clotrimazole. The compounds demonstrated excellent to weak antifungal activity. Among the synthesized derivatives, 4f and 4h showed significant activity and 4c exhibited moderate activity against Candida albicans, Candida tropicalis and Aspergillus niger as compared with the standard antifungal agent - clotrimazole. The minimum inhibitory concentration of the compounds was in the range of 1.62-25 microg/mL against fungi. Furthermore, the substitution of chloro, nitro and methoxy groups at para position of benzene moiety play an important role in enhancing the antifungal activity of this class of compounds.
... The data reported in this article may be helpful to the medicinal chemists who are working in... more ... The data reported in this article may be helpful to the medicinal chemists who are working in this area. REFERENCES 1. Vipin K., Archana S., Prabodh CS: J. Enzyme Inhib. Med. Chem. 26, 198 (2011). 2. Sumru O., Fusun, K., Yamur T.: J. Enzyme Inhib. Med. Chem. ...
A series of (E)-N'-(substituted benzylidene)isonicotinohydrazide derivatives were synthesized... more A series of (E)-N'-(substituted benzylidene)isonicotinohydrazide derivatives were synthesized by coupling isoniazid with differently substituted aldehydes and benzophenones in the presence of absolute ethanol along with catalytic amount of glacial acetic acid. The structure of all the synthesized compounds were confirmed and characterized by using various spectral technique like IR, 1H NMR, 13C NMR and mass spectroscopy. All the synthesized compounds were evaluated for their antimicrobial activity in terms of zone of inhibition, minimum inhibitory concentration, minimum bactericidal concentration and minimum fungicidal concentration in camparison to the standard drugs. The results revealed that all synthesized compounds had shown potent to mild biological activity. Among the synthesized derivatives, (E)-N'-(3,4-dimethoxybenzylidene)isonicotinohydrazide 2e, (E)-N'-(3,4,5-trimethoxybenzylidene)isonicotinohydrazide 2f and (E)-N'-(4-hydroxy-3-methoxybenzylidene)isonicoti...
Irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) are ... more Irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) are highly prevalent gastrointestinal disorders. Traditional symptoms based therapies had somewhat limited success and efficacy in addressing the disorders. Recently, linaclotide emerged as novel peptide capable of improving abdominal symptoms in patients suffering from IBS-C and CIC. Guanylate cyclase C (GC-C) receptor a multi domain protein, found to be molecular target for linaclotide which acts by activating GC-C receptor on the apical surface of intestinal epithelial cells. Binding of linaclotide to GC-C receptor triggers the elevation of second messenger cGMP that elicits fluid secretion into intestinal cells which play a critical role in maintaining homeostasis through cystic fibrosis transmembrane conductance regulator (CFTR). Data from Phase II and III clinical trials demonstrated that linaclotide seems to produce a statistically significant increase in stool frequency, improved str...
ABSTRACT Reduced levels of c-aminobutyric acid (GABA) are cause of quite a many diseases, and it ... more ABSTRACT Reduced levels of c-aminobutyric acid (GABA) are cause of quite a many diseases, and it cannot be directly introduced into the body to enhance its level because of the blood–brain barrier. Thus the technique used for the purpose involves the inhibition of aminobutyrate transaminase (ABAT), the enzyme catalyzing its degradation. The structure of human ABAT is not currently known experimentally, thus, it was predicted by homology modeling using pig ABAT as template due to high level of sequence similarity and conservation. A series of new c-aminobutyric acid (GABA) derivatives obtained from 4-(1,3-dioxoisoindolin-2-yl)butanoic acid are used in this study. These c -aminobutyric acid (GABA) derivatives were used as ligand dockings against human ABAT as well as pig ABAT receptors
Twelve compounds belonging to series 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)-N-[4-oxo-2-(substitute... more Twelve compounds belonging to series 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)-N-[4-oxo-2-(substituted)phenyl-1,3-thiazolidin-3-yl]acetamide (5a-l) were synthesized. These compounds were evaluated for theirin-vitroantibacterial againstE. coli, S. aureus, K. pneumoniae, P. aeruginosa & antifungalactivity againstC. albicans, A. niger & A. flavusby cup-plate method. Structures of all the newly synthesized compounds were confirmed by elemental analysis,1H-NMR & FT-IR spectral data interpretation. Compounds 5d & 5h having p-nitrophenyl &p-trifluoromethylphenyl group respectively on 2-position of thiazolidinone ring attached to N-atom of acetamido group on 1-position of 3-methyl-1H-quinoxaline-2-one, were found to be active against all the bacterial…
... ewsletter Arora et al. 659 Current Trends in Anticonvulsant 4(3H)-quinazolinone: A Review Din... more ... ewsletter Arora et al. 659 Current Trends in Anticonvulsant 4(3H)-quinazolinone: A Review Dinesh Arora, Hitesh Kumar*, Dipan Malhotra, Manav Malhotra ... & Therapeutics. 2005; 105: 229 – 266. 7. Gupta YK, Malhotra J. Antiepileptic drug therapy in the twenty first century. Ind. ...
Background: 5α-Reductase (5AR), an NADPH dependent enzyme, is expressed in most of the prostate e... more Background: 5α-Reductase (5AR), an NADPH dependent enzyme, is expressed in most of the prostate epithelial cells. By converting testosterone (T) into more potent androgen dihydrotestosterone (DHT), it plays an important role in men physiology and represents an efficient therapeutic target for androgen-dependent diseases. Over the last few years, significant efforts have been made in order to develop 5AR inhibitors (5ARI) to treat Benign Prostatic Hyperplasia because of excessive production of DHT. Methods: In the present study, 2D and 3D QSAR pharmacophore models have been generated for 5ARI based on known IC50 values with extensive validations. The four featured 2D pharmacophore based PLS model correlated the topological interactions (SsOHE-index); semi empirical (Quadrupole2) and physicochemical descriptors (Mol. Wt, Bromines Count, Chlorines Count) with 5AR inhibitory activity, and has the highest correlation coefficient (r2 = 0.98, q2 =0.84; F = 57.87, pred r2 = 0.88). Internal ...
Convolvulus arvensis is a long lived deep rooted weed belongs to the family Convolvulaceae. It is... more Convolvulus arvensis is a long lived deep rooted weed belongs to the family Convolvulaceae. It is commonly known as European bindweed, bindweed, creeping jenny, morning glory, and devil’s guts. It has at least 84 common names. Field bindweed is found in a wide range of habitats: orchards, vineyards, roadsides, ditch banks, cropland, steam banks, and lakeshores. Field bindweed begins growing in the late spring or early summer and may persist until the first frost. It is most likely confused with the Ipomoea spp., Calystegia spp., Dioscorea spp, Polygonum convolvulus L. It is very much difficult to differentiate between all these species. The plant contains Saponins, Alkaloids, and Polyphenolic compounds Flavonoids and Tannins. It has stimulant, anti-oxidant, anticancer and laxative effect. This review shows its identification, some of the isolated compounds and its biological activities.
Steroids have contributed a lot in the development of organic chemistry. The broad operations of ... more Steroids have contributed a lot in the development of organic chemistry. The broad operations of biological activity and multiplicity of action make steroids one of the most intriguing classes of biologically active compounds. The area has been very fascinating for the study of reaction mechanisms and stereochemistry and a brief discussion on neuromuscular blocking agents is discussed below.
Chronic myelogenous leukaemia is one of the major chronic myeloproliferative diseases of pluipote... more Chronic myelogenous leukaemia is one of the major chronic myeloproliferative diseases of pluipotential haematopoietic stem cells. Many therapeautic agents have failed to provide any relief to the patients suffering from chronic myelogenous leukaemia (CML). Imatinib was first ever developed drug for the treatment of (CML) but the problem associated with it is the resistant against this drug. Therefore, the development of new agents will remain an important challenging task for medicinal chemists. So, there is an urgent need for identification of new, potent, and less toxic agents which ideally shorten the duration of therapy and are effective against CML. Nilotinib which are found to be effective in patient with Imatinib – resistant chronic myelogenous leukaemia (CML). It is a second generation BCR-ABL tyrosine kinase inhibitor and found to be target specific kinase inhibitor as compare with Imatinib. This reviews article reflects development of Nolotinib, mechanism of action, precli...
From the recent studies, 3,5-dibenzoyl-1,4-dihydropyridone (DHP) derivatives, DP-7, has emerged a... more From the recent studies, 3,5-dibenzoyl-1,4-dihydropyridone (DHP) derivatives, DP-7, has emerged as a potent multidrug reverting agent that inhibits efflux of drug from cell wall by inhibiting the activity of ATP Binding Cassettes. On the other hand, dihydropyrimidine (DHPM) derivative, (aza analogue) namely, monastrol inhibits the protein Eg5, which is responsible for the separation of daughter chromosomes during cell division and controls the growth of the tumor cells. In the present report, we have reported the hybridize molecules of these two potent molecules to check the dual action in cancer chemotherapy by synthesizing various thio and oxo analogues, bearing substituted aryl groups at 4th position of the DHPM ring. The newly synthesized molecules were screened for antiproliferative effects in mdr1-gene transfected mouse lymphoma cell line (l5178 y). Among these newly synthesized compounds namely, II h, I g, I i, and I j showed a very potent antiproliferative activity.
17-aza steroids are the important class of compounds used as 5α-reductase inhibitors for the trea... more 17-aza steroids are the important class of compounds used as 5α-reductase inhibitors for the treatment of benign prostatichyperplasia. As these agents blocks the conversion of Testosterone (T) into Dihydrotestosterone (DHT) which is the mainreason for the development of benign prostatic hyperplasia. Benign prostatic hyperplasia (BPH) is the noncancerousproliferation of the prostate gland associated with benign prostatic obstruction and lower urinary tract symptoms (LUTS)such as frequency, hesitancy and urgency. Its prevalence increases with age affecting around 70% by the age of 70 years.Main attention given to the 17-aza steroids is due to the back binding or inverted action that was proposed by Mac Donald et al. In this review, different 17-aza steroids such as seco-steroids, alkyl chain derivates at 17-position, 3β-esters and many other derivatives were shown.
International Journal of Pharmacognosy and Phytochemical Research
We herein report the synthesis of 3β-substituted amides of 17a-aza-D-homo-4-androsten-17-one (11a... more We herein report the synthesis of 3β-substituted amides of 17a-aza-D-homo-4-androsten-17-one (11a-11r) from commercially available Diosgenin as the starting material. The structures of newly synthesized compounds were confirmed by IR, (1)H NMR, (13)C NMR and mass spectrometry. All the synthesized analogues were tested for their 5α- reductase inhibitory and antimicrobial activity, some of them exhibit moderate to potent activity comparable to the reference drugs. Among the synthesized derivatives the analogue (11r) 3β-(indonlylbutanamido)-17a-aza-D-homo-4- androsten-17-one was found to be active against both 5α-reductase enzyme and microbial strains, whereas the analogue (11i) 3β-(3,4-dimethoxy-benzamido)-17a-aza-D-homo-4-androsten-17-one was found to be the least active. The detailed 5α-reductase inhibitors and antimicrobial activities of the synthesized compounds were reported.
In the present study, (E)-2-{ [-2-(2,4-Dinitrophenyl)hydrazono]methyl} phenol (3) was synthesized... more In the present study, (E)-2-{ [-2-(2,4-Dinitrophenyl)hydrazono]methyl} phenol (3) was synthesized and used as key intermediate for the synthesis of new Mannich bases. All the synthesized compounds were evaluated for their antifungal activity against three fungal strains Candida albicans, Candida tropicalis and Aspergillus niger and antioxidant activity. The structure of these compounds was confirmed by IR, 1H NMR and 13C NMR studies. Most of the compounds exhibited moderate to significant activities.
A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by ... more A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by coupling it with different substituted aldehydes, acetophenone, and benzophenones in presence of absolute ethanol along with catalytic amount of glacial acetic acid. All the synthesized compound were confirmed and characterized by using various spectral technique like IR, 1H NMR, 13C NMR, and mass spectroscopy studies. Anticonvulsant evaluations of all the synthesized compounds were done using various seizures models like maximal electroshock-induced seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) at a dose of 30, 100, and 300 mg/kg body weight and anticonvulsant activity was noted at 0.5 h and 4 h time intervals after the drug administration. Compound 1a (E)-N′-2-benzylidene isonicotinohydrazide, 1g (E)-N′-2-ethoxybenzylidene isonicotinohydrazide, 1k (E)-N′-3-flourobenzylidene isonicotinohydrazide and 3a (E)-N′-diphenylmethylene isonicotinohydrazide showed protection in MES mo...
In the present study, a series of (Z)-N-(1-[2-{3-[(dimethylamino)methyl)]-2-methoxyphenyl}-5-(pyr... more In the present study, a series of (Z)-N-(1-[2-{3-[(dimethylamino)methyl)]-2-methoxyphenyl}-5-(pyridin-4-yl)-1,3,4-oxadiazol-3(2H)-yl]ethylidene)benzenamine derivatives have been synthesized and characterized by IR, 1H NMR and 13C NMR spectra. All the synthesized compounds were evaluated for their antifungal activity and were compared with the standard drug, clotrimazole. The compounds demonstrated excellent to weak antifungal activity. Among the synthesized derivatives, 4f and 4h showed significant activity and 4c exhibited moderate activity against Candida albicans, Candida tropicalis and Aspergillus niger as compared with the standard antifungal agent - clotrimazole. The minimum inhibitory concentration of the compounds was in the range of 1.62-25 microg/mL against fungi. Furthermore, the substitution of chloro, nitro and methoxy groups at para position of benzene moiety play an important role in enhancing the antifungal activity of this class of compounds.
... The data reported in this article may be helpful to the medicinal chemists who are working in... more ... The data reported in this article may be helpful to the medicinal chemists who are working in this area. REFERENCES 1. Vipin K., Archana S., Prabodh CS: J. Enzyme Inhib. Med. Chem. 26, 198 (2011). 2. Sumru O., Fusun, K., Yamur T.: J. Enzyme Inhib. Med. Chem. ...
A series of (E)-N'-(substituted benzylidene)isonicotinohydrazide derivatives were synthesized... more A series of (E)-N'-(substituted benzylidene)isonicotinohydrazide derivatives were synthesized by coupling isoniazid with differently substituted aldehydes and benzophenones in the presence of absolute ethanol along with catalytic amount of glacial acetic acid. The structure of all the synthesized compounds were confirmed and characterized by using various spectral technique like IR, 1H NMR, 13C NMR and mass spectroscopy. All the synthesized compounds were evaluated for their antimicrobial activity in terms of zone of inhibition, minimum inhibitory concentration, minimum bactericidal concentration and minimum fungicidal concentration in camparison to the standard drugs. The results revealed that all synthesized compounds had shown potent to mild biological activity. Among the synthesized derivatives, (E)-N'-(3,4-dimethoxybenzylidene)isonicotinohydrazide 2e, (E)-N'-(3,4,5-trimethoxybenzylidene)isonicotinohydrazide 2f and (E)-N'-(4-hydroxy-3-methoxybenzylidene)isonicoti...
Irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) are ... more Irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) are highly prevalent gastrointestinal disorders. Traditional symptoms based therapies had somewhat limited success and efficacy in addressing the disorders. Recently, linaclotide emerged as novel peptide capable of improving abdominal symptoms in patients suffering from IBS-C and CIC. Guanylate cyclase C (GC-C) receptor a multi domain protein, found to be molecular target for linaclotide which acts by activating GC-C receptor on the apical surface of intestinal epithelial cells. Binding of linaclotide to GC-C receptor triggers the elevation of second messenger cGMP that elicits fluid secretion into intestinal cells which play a critical role in maintaining homeostasis through cystic fibrosis transmembrane conductance regulator (CFTR). Data from Phase II and III clinical trials demonstrated that linaclotide seems to produce a statistically significant increase in stool frequency, improved str...
ABSTRACT Reduced levels of c-aminobutyric acid (GABA) are cause of quite a many diseases, and it ... more ABSTRACT Reduced levels of c-aminobutyric acid (GABA) are cause of quite a many diseases, and it cannot be directly introduced into the body to enhance its level because of the blood–brain barrier. Thus the technique used for the purpose involves the inhibition of aminobutyrate transaminase (ABAT), the enzyme catalyzing its degradation. The structure of human ABAT is not currently known experimentally, thus, it was predicted by homology modeling using pig ABAT as template due to high level of sequence similarity and conservation. A series of new c-aminobutyric acid (GABA) derivatives obtained from 4-(1,3-dioxoisoindolin-2-yl)butanoic acid are used in this study. These c -aminobutyric acid (GABA) derivatives were used as ligand dockings against human ABAT as well as pig ABAT receptors
Twelve compounds belonging to series 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)-N-[4-oxo-2-(substitute... more Twelve compounds belonging to series 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)-N-[4-oxo-2-(substituted)phenyl-1,3-thiazolidin-3-yl]acetamide (5a-l) were synthesized. These compounds were evaluated for theirin-vitroantibacterial againstE. coli, S. aureus, K. pneumoniae, P. aeruginosa & antifungalactivity againstC. albicans, A. niger & A. flavusby cup-plate method. Structures of all the newly synthesized compounds were confirmed by elemental analysis,1H-NMR & FT-IR spectral data interpretation. Compounds 5d & 5h having p-nitrophenyl &p-trifluoromethylphenyl group respectively on 2-position of thiazolidinone ring attached to N-atom of acetamido group on 1-position of 3-methyl-1H-quinoxaline-2-one, were found to be active against all the bacterial…
... ewsletter Arora et al. 659 Current Trends in Anticonvulsant 4(3H)-quinazolinone: A Review Din... more ... ewsletter Arora et al. 659 Current Trends in Anticonvulsant 4(3H)-quinazolinone: A Review Dinesh Arora, Hitesh Kumar*, Dipan Malhotra, Manav Malhotra ... & Therapeutics. 2005; 105: 229 – 266. 7. Gupta YK, Malhotra J. Antiepileptic drug therapy in the twenty first century. Ind. ...
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