Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
VOLUME: 8
ISSUE: 5
DOI: 10.2174/157018011795514212 Price: $58
ISSN (Online): 1875-628X
VOLUME: 8
ISSUE: 5
DOI: 10.2174/157018011795514212 Price: $58
Novel 2-(benzo[d]thiazol-2-yl)-1-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl)ethanone Derivatives: Synthesis and Antibacterial Activity
Author(s):
Chun-Xiu Pan, Jun Li and Xin-Hua Liu
Pages 459-463 (5)
Pages 459-463 (5)
Abstract:
A series of novel 2-(benzo[d]thiazol-2-yl)-1-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl)ethanone derivatives were synthesized and characterized by NMR, ESI-MS. Biological activity tests results show that compounds 4a, 4b, 4d and 4g displayed activity with MIC of 1.562 μg/mL against B. subtilis ATCC 6633, compound 4d displayed significant activity with MIC of 1.562 μg/mL against S. aureus ATCC 6538. Compound 4a with potent antibacterial activities strongly inhibited S. aureus DNA gyrase and B. subtilis DNA gyrase with IC50s of 0.5 μg/ml against S. aureus DNA gyrase and B. subtilis DNA gyrase.
Keywords:
Benzo[d]thiazole, Dihydropyrazole, Antibacterial activity, ethanone Derivatives, C-glycoside, pyrazole, Staphylococcus, bromination, acetophenone, benzothiazole, aeruginosa, Novobiocin
Affiliation:
School of Pharmacy, Anhui Medical University, Hefei, 230032, P. R. China.