Ashish P. Keche

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Structure-activity relationship studies were carried out for lead generation following structure-guided design approach from an isocytosine scaffold identified earlier for xanthine oxidase inhibition. A 470-fold improvement in in vitro IC(50) was obtained in the process. Five most potent compounds with nanomolar IC(50) values were selected for(More)
A series of novel 1-acetyl-3-(3,4-dimethoxypheny)-5-(4-(3-(arylureido/arylthioureido/arylsulfonamido) phenyl)-4,5-dihydropyrazole derivatives of biological interest have been prepared by sequential cyclization of 1-(4-nitrophenyl)-3-(3,4-dimethoxyphenyl)-pro-2-ene-1 with hydrazine hydrate, reduction followed by reaction of resulting amine with different(More)
A series of novel 4-(3-(trifluoromethyl)phenylamino-6-(4-(3-arylureiodo/arylthioureido/arylsulfonamido)-pyrimidine derivatives of biological interest were prepared by the sequential Suzuki cross coupling, acid amination, reduction followed by reaction of resulting amine with different arylisocyantes or arylisothiocyantes or arylsulfonyl chlorides. All the(More)
A series of novel thiourea analogs of 3,4-dihydropyrimidin-2(1-H)-one derivatives of biological interest were prepared by sequential Bigineli’s reaction, reduction followed by reaction of resulting amine with different arylisothiocynates. All the synthesized compounds (1–23) were screened against the proinflammatory cytokines (TNF-α and IL-6) and(More)
A series of novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of biological interest were prepared by sequential Bigineli's reaction, reduction followed by reaction of resulting amines with different arylisocynates. All the synthesized (1-23) compounds were screened against the pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity(More)
A series of substituted N-(quinolin-4-yl)ethanediamine phenyl urea derivatives of biological interest were prepared by sequential quinoline synthesis, chlorination, and substitution reaction followed by reaction of resulting amine with different aryl isocyanates. All synthesized compounds (1–13) were screened for their pro-inflammatory cytokines (TNF-α and(More)
A new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives were synthesized using simple three component condensation, reduction, and nucleophilic addition sequence in moderate to good yields. All the synthesized compounds 6a–j were evaluated for their anti-inflammatory [against the pro-inflammatory cytokines (tumor necrosis factor-alpha,(More)
A series of novel 3-hydroxy-2-(2,4,5-trimethoxyphenyl)-4H-chromen-4-one (flavonol) derivatives (2a–u) of biological interest have been prepared via CLAISEN–SCHMIDT condensation followed by ALGAR–FLYNN–OYAMADA reaction and to search for the potent nonsteroidal anti-inflammatory agents from this novel series. All the synthesized compounds have been screened(More)
A series of novel 6-methoxy-2-(piperazin-1-yl)-4H-chromen-4-one and 5,7-dimethoxy-2-(piperazin-1-ylmethyl)-4H-chromen-4-one derivatives of biological interest were prepared and screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Among all the compound screened (5a-j and 10k-t), the(More)
We report synthesis of novel series of amino alcohol derivatives of 2-methyl benzimidazole. These compounds have been synthesized by epoxide ring opening of 2-methyl benzimidazole with different substituted cyclic amines. These synthesized compounds have been characterized using IR, H NMR and ES-MS spectral data together with their melting point. These(More)