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, Xin-Hua Liu

Journal Name: Letters in Drug Design & Discovery

Volume 8 , Issue 5 , 2011

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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

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Article Details

Year: 2011
Page: [459 - 463]
Pages: 5
DOI: 10.2174/157018011795514212
Price: $65

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