Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 23, Issue 2, Pages 882-895Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-013-0679-0
Keywords
Pyrazolylpyrazolines; Chalcones; Antimicrobial activity; Anti-inflammatory activity; Benzenesulfonamide
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Funding
- Defence Research and Development Organization (DRDO), New Delhi
- Council of Scientific and Industrial Research (CSIR), New Delhi
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Two novel series of pyrazolylpyrazolines (4a-i and 5a-i) bearing benzenesulfonamide moiety at position-1 of pyrazole were synthesized by the reaction of appropriate chalcones (3a-i) with hydrazine hydrate or 4-hydrazinobenzenesulfonamide hydrochloride in refluxing ethanol/THF containing catalytic amount of acetic acid. All the newly synthesized target compounds (4a-i and 5a-i) were screened for in vivo anti-inflammatory (AI) activity using carrageenan-induced rat paw edema assay. In addition, all 18 synthesized compounds were evaluated for in vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria, and in vitro antifungal activity against two fungal strains. The results revealed that seven compounds (4b-e, 4g, 5e, and 5i) displayed excellent AI activity (>= 70 % inhibition) including two compounds (4b and 4e) which showed same level of AI activity as that of the standard drug indomethacin (78 % inhibition) 3 h after carrageenan injection. In addition, most of the compounds exhibited moderate antibacterial activity against Gram-positive bacteria as well as moderate antifungal activity against the tested fungi.
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