Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 21, Pages 6611-6615Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.08.118
Keywords
1-Acetyl-3,5-diaryl-4,5-dihydro (1H) pyrazole; Urea; Thiourea and sulfonamide derivatives; Anti-inflammatory; Anti-bacterial; Anti-fungal
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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-alpha 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-alpha and 76-93% IL-6 inhibitory activity) at concentration of 10 mu M with reference to standard dexamethasone (76% TNF-alpha and 86% IL-6 inhibitory activity at 1 mu M). Compounds 24, 26, 27, 28 and 29 exhibited promising antimicrobial activity at MIC values ranging from 70 to 10 mu g/mL against all the selected pathogenic bacteria and fungi. (C) 2012 Elsevier Ltd. All rights reserved.
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