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Keche A.P.,Maharashtra Udaygiri Mahavidayla | Hatnapure G.D.,Maharashtra Udaygiri Mahavidayla | Tale R.H.,Srtm University | Rodge A.H.,Srtm University | And 2 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

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 arylisocyanates or arylisothiocyanates or arylsulfonyl chlorides. All the synthesized compounds (1-32) have been screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological evaluation study showed, the compounds 4, 5, 9, 11, 14 and 16 found to have promising anti-inflammatory activity (up to 61-85% TNF-α and 76-93% IL-6 inhibitory activity) at concentration of 10 μM with reference to standard dexamethasone (76% TNF-α and 86% IL-6 inhibitory activity at 1 μM). Compounds 24, 26, 27, 28 and 29 exhibited promising antimicrobial activity at MIC values ranging from 70 to 10 μg/mL against all the selected pathogenic bacteria and fungi. © 2012 Elsevier Ltd. All rights reserved. Source


Hatnapure G.D.,Maharashtra Udaygiri Mahavidayla | Keche A.P.,Maharashtra Udaygiri Mahavidayla | Rodge A.H.,Srtm University | Birajdar S.S.,Maharashtra Udaygiri Mahavidayla | And 3 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

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 compounds 5c, 5g, 5h, 10l, 10m, 10n and 10r found to have promising anti-inflammatory activity (up to 65-87% TNF-α and 70-93% IL-6 inhibitory activity) at concentration of 10 μM with reference to standard dexamethasone (71% TNF-a and 84% IL-6 inhibitory activities at 1 μM) while the compounds 5b, 5i, 5j, 10s and 10t found to be potent antimicrobial agent showing even 2 to 2.5-fold more potency than that of standard ciprofloxacin and miconazole at the same MIC value of 10 μg/mL. © 2012 Elsevier Ltd. All rights reserved. Source


Keche A.P.,Maharashtra Udaygiri Mahavidayla | Hatnapure G.D.,Maharashtra Udaygiri Mahavidayla | Tale R.H.,iversity | Rodge A.H.,iversity | And 3 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

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 synthesized compounds (1-25) were screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological data revealed that among all the compounds screened, compounds 5, 6, 11, 12, 16 and 20 were found to have moderate to potent anti-inflammatory activity (up to 48-78% TNF-α and 56-96% IL-6 inhibitory activity) with reference to standard dexamethasone at 10 μM. The compounds 10, 12, 13, 18, 20, 22, 24 and 25 found to have promising antimicrobial activity against all the selected pathogenic bacteria and fungi. © 2012 Elsevier Ltd. All rights reserved. Source

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