kishor Jain - Academia.edu (original) (raw)
Papers by kishor Jain
Journal of Heterocyclic Chemistry, Mar 1, 1984
Reactions d'amino-2 thiophenecarboxylates-3 d'ethyle substitues dimethyl-4,5, tetramethyl... more Reactions d'amino-2 thiophenecarboxylates-3 d'ethyle substitues dimethyl-4,5, tetramethylene-4,5 ou aza-3tetramethylene-4,5 avec des cyanates, thiocyanates, cyanures d'acyle, ou acetonitriles α-fonctionnalises: obtention de thieno [2,3-d] pyrimidones-4 disubstituees 5,6 et de thieno [3,2-d] pyrimidones-4 disubstituees 6,7
Medicinal Chemistry Research, Dec 24, 2011
ABSTRACT From the recent studies, 3,5-dibenzoyl-1,4-dihydropyridone (DHP) derivatives, DP-7, has ... more ABSTRACT 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.
Journal of Heterocyclic Chemistry, Mar 1, 1993
The reaction of N‐arylcyanamides with thiophene o‐aminonitriles under the influence of dry hydrog... more The reaction of N‐arylcyanamides with thiophene o‐aminonitriles under the influence of dry hydrogen chloride gas yields a mixture of two products. The major product has been identified as 2‐amino‐3‐aryl‐4‐iminothieno[2,3‐d]pyrimidine and the minor as 2‐amino‐3‐arylthieno[2,3‐H]pyrimidin‐4(3H)‐one.
European journal of medicinal chemistry, Apr 1, 2014
A small, focussed library of condensed 2H-4-arylaminopyrimidines, with 3-diversity points, based ... more A small, focussed library of condensed 2H-4-arylaminopyrimidines, with 3-diversity points, based on an initial design by molecular docking study of this scaffold at the active site of the fungal enzyme of cytochrome P450 family, lanosterol 14α-demethylase (CYP51) was synthesized through a one-pot green chemical synthetic protocol. The screening of the synthesised compounds for antifungal activity against Candida albicans, Aspergillus fumigatus &Aspergillus niger revealed activity in many of the compounds as comparable to that of fluconazole. Based on the antifungal activity and physicochemical property data of these derivatives, a meaningful SAR has been proposed.
ChemInform, Apr 15, 2008
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
![Research paper thumbnail of Synthesis and antihyperlipidemic activity of some novel 4-substituted-2-substitutedmethyltriazino[6,1-b]quinazolin-10-ones and 2,4-disubstituted-6,7-dimethoxy quinazoline](https://attachments.academia-assets.com/120484062/thumbnails/1.jpg)
](Arabian Journal of Chemistry, Sep 1, 2016
International Journal of Green Pharmacy, 2008
Aquilaria agallocha Roxb, family, Th ymelaeaceae, is an evergreen plant of India, China and Tibet... more Aquilaria agallocha Roxb, family, Th ymelaeaceae, is an evergreen plant of India, China and Tibet, commonly described as aloe wood or agarwood. Traditionally, the bark, root and heartwood are used for their medicinal properties as a folk medicine to treat infl ammation, arthritis, vomiting, cardiac disorders, cough, asthma, leprosy, anorexia, headache and gout. Th e present study was carried out to investigate the antioxidant activity of ethyl acetate extract of Aquilaria agallocha (EAA). EAA was tested in vitro at diff erent concentrations for inhibitory eff ect on nitrite-induced oxidation of haemoglobin in human blood haemolysate. Results indicate a strong antioxidant eff ect of EAA in a concentration range of 500-3500 μg/ml. However pro-oxidant activity was observed at higher concentrations of these compounds. Key words: Antioxidant, Aquilaria agallocha, methaemoglobin, nitrite-radical
Heterocycles, 2009
The single pot facile reaction of a host of nitriles with a variety of o-aminocarbonyl substrates... more The single pot facile reaction of a host of nitriles with a variety of o-aminocarbonyl substrates of benzene, thiophene, benzothiophene, pyridothiophene, furan, pyrrole, pyridopyrazole, naphthopyran etc., to form corresponding condensed pyrimidines functionalized at 2-and ...
![Research paper thumbnail of Determination of 4-Chloro-2-chloromethyl-5-(4-chlorophenyl)thieno[2,3-d]- pyrimidine in Rabbit Serum by HPLC and its Application in a Pharmacokinetic Study](https://attachments.academia-assets.com/120484057/thumbnails/1.jpg)
](Indian Journal of Pharmaceutical Education and Research, 2013
Journal of Heterocyclic Chemistry, Feb 1, 1990
Condensation of a nitrile with benzene, furan and thiophene ortho‐aminonitriles in the presence o... more Condensation of a nitrile with benzene, furan and thiophene ortho‐aminonitriles in the presence of dry hydrogen chloride yields condensed 4‐chloropyrimidines, condensed 4‐aminopyrimidines or a mixture of the two condensed pyrimidines in varying proportions depending upon the nature of the nitrile and the substrate, ortho‐aminonitrile.
Medicinal Chemistry Research, Dec 4, 2012
Archiv Der Pharmazie, Oct 20, 2013
ChemInform, 1989
Twenty‐five title compounds of type (III) are prepared as potential antimalarial drugs.
Drug design and discovery, 1997
The present study describes the synthesis and quantitative structure activity relationships (QSAR... more The present study describes the synthesis and quantitative structure activity relationships (QSAR) of novel 3-amino-2-(substituted)aminomethyl-5,6-disubstitutedthieno[2,3-d] pyrimidin-4(3H)-ones for their potent H1-receptor antagonist activity on the guinea pig ileum. With the IC50 values in the range of 10(-5) gms/lit, all the compounds tested were found to possess ten fold higher affinity to the H1-receptor than diphenhydramine and cetirizine, but lower than astemizole and loratidine. The sedative potential of these compounds was found to be lower than cetirizine and astemizole but comparable to loratidine. The QSAR study indicates a parabolic relationship of the biological activity mainly with the steric parameters and partly with the lipophilic parameters.
Journal of Heterocyclic Chemistry, 1984
Reactions d'amino-2 thiophenecarboxylates-3 d'ethyle substitues dimethyl-4,5, tetramethyl... more Reactions d'amino-2 thiophenecarboxylates-3 d'ethyle substitues dimethyl-4,5, tetramethylene-4,5 ou aza-3tetramethylene-4,5 avec des cyanates, thiocyanates, cyanures d'acyle, ou acetonitriles α-fonctionnalises: obtention de thieno [2,3-d] pyrimidones-4 disubstituees 5,6 et de thieno [3,2-d] pyrimidones-4 disubstituees 6,7
Journal of Heterocyclic Chemistry, Mar 1, 1984
Reactions d'amino-2 thiophenecarboxylates-3 d'ethyle substitues dimethyl-4,5, tetramethyl... more Reactions d'amino-2 thiophenecarboxylates-3 d'ethyle substitues dimethyl-4,5, tetramethylene-4,5 ou aza-3tetramethylene-4,5 avec des cyanates, thiocyanates, cyanures d'acyle, ou acetonitriles α-fonctionnalises: obtention de thieno [2,3-d] pyrimidones-4 disubstituees 5,6 et de thieno [3,2-d] pyrimidones-4 disubstituees 6,7
Medicinal Chemistry Research, Dec 24, 2011
ABSTRACT From the recent studies, 3,5-dibenzoyl-1,4-dihydropyridone (DHP) derivatives, DP-7, has ... more ABSTRACT 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.
Journal of Heterocyclic Chemistry, Mar 1, 1993
The reaction of N‐arylcyanamides with thiophene o‐aminonitriles under the influence of dry hydrog... more The reaction of N‐arylcyanamides with thiophene o‐aminonitriles under the influence of dry hydrogen chloride gas yields a mixture of two products. The major product has been identified as 2‐amino‐3‐aryl‐4‐iminothieno[2,3‐d]pyrimidine and the minor as 2‐amino‐3‐arylthieno[2,3‐H]pyrimidin‐4(3H)‐one.
European journal of medicinal chemistry, Apr 1, 2014
A small, focussed library of condensed 2H-4-arylaminopyrimidines, with 3-diversity points, based ... more A small, focussed library of condensed 2H-4-arylaminopyrimidines, with 3-diversity points, based on an initial design by molecular docking study of this scaffold at the active site of the fungal enzyme of cytochrome P450 family, lanosterol 14α-demethylase (CYP51) was synthesized through a one-pot green chemical synthetic protocol. The screening of the synthesised compounds for antifungal activity against Candida albicans, Aspergillus fumigatus &Aspergillus niger revealed activity in many of the compounds as comparable to that of fluconazole. Based on the antifungal activity and physicochemical property data of these derivatives, a meaningful SAR has been proposed.
ChemInform, Apr 15, 2008
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Arabian Journal of Chemistry, Sep 1, 2016
International Journal of Green Pharmacy, 2008
Aquilaria agallocha Roxb, family, Th ymelaeaceae, is an evergreen plant of India, China and Tibet... more Aquilaria agallocha Roxb, family, Th ymelaeaceae, is an evergreen plant of India, China and Tibet, commonly described as aloe wood or agarwood. Traditionally, the bark, root and heartwood are used for their medicinal properties as a folk medicine to treat infl ammation, arthritis, vomiting, cardiac disorders, cough, asthma, leprosy, anorexia, headache and gout. Th e present study was carried out to investigate the antioxidant activity of ethyl acetate extract of Aquilaria agallocha (EAA). EAA was tested in vitro at diff erent concentrations for inhibitory eff ect on nitrite-induced oxidation of haemoglobin in human blood haemolysate. Results indicate a strong antioxidant eff ect of EAA in a concentration range of 500-3500 μg/ml. However pro-oxidant activity was observed at higher concentrations of these compounds. Key words: Antioxidant, Aquilaria agallocha, methaemoglobin, nitrite-radical
Heterocycles, 2009
The single pot facile reaction of a host of nitriles with a variety of o-aminocarbonyl substrates... more The single pot facile reaction of a host of nitriles with a variety of o-aminocarbonyl substrates of benzene, thiophene, benzothiophene, pyridothiophene, furan, pyrrole, pyridopyrazole, naphthopyran etc., to form corresponding condensed pyrimidines functionalized at 2-and ...
Indian Journal of Pharmaceutical Education and Research, 2013
Journal of Heterocyclic Chemistry, Feb 1, 1990
Condensation of a nitrile with benzene, furan and thiophene ortho‐aminonitriles in the presence o... more Condensation of a nitrile with benzene, furan and thiophene ortho‐aminonitriles in the presence of dry hydrogen chloride yields condensed 4‐chloropyrimidines, condensed 4‐aminopyrimidines or a mixture of the two condensed pyrimidines in varying proportions depending upon the nature of the nitrile and the substrate, ortho‐aminonitrile.
Medicinal Chemistry Research, Dec 4, 2012
Archiv Der Pharmazie, Oct 20, 2013
ChemInform, 1989
Twenty‐five title compounds of type (III) are prepared as potential antimalarial drugs.
Drug design and discovery, 1997
The present study describes the synthesis and quantitative structure activity relationships (QSAR... more The present study describes the synthesis and quantitative structure activity relationships (QSAR) of novel 3-amino-2-(substituted)aminomethyl-5,6-disubstitutedthieno[2,3-d] pyrimidin-4(3H)-ones for their potent H1-receptor antagonist activity on the guinea pig ileum. With the IC50 values in the range of 10(-5) gms/lit, all the compounds tested were found to possess ten fold higher affinity to the H1-receptor than diphenhydramine and cetirizine, but lower than astemizole and loratidine. The sedative potential of these compounds was found to be lower than cetirizine and astemizole but comparable to loratidine. The QSAR study indicates a parabolic relationship of the biological activity mainly with the steric parameters and partly with the lipophilic parameters.
Journal of Heterocyclic Chemistry, 1984
Reactions d'amino-2 thiophenecarboxylates-3 d'ethyle substitues dimethyl-4,5, tetramethyl... more Reactions d'amino-2 thiophenecarboxylates-3 d'ethyle substitues dimethyl-4,5, tetramethylene-4,5 ou aza-3tetramethylene-4,5 avec des cyanates, thiocyanates, cyanures d'acyle, ou acetonitriles α-fonctionnalises: obtention de thieno [2,3-d] pyrimidones-4 disubstituees 5,6 et de thieno [3,2-d] pyrimidones-4 disubstituees 6,7