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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Novel 4-bromo-2-(3-methyl-1-(substituted-phenylsulfonyl)-4,5-dihydro-1- H-pyrazol-5-yl)phenol Derivatives: Synthesis and Antibacterial Activity

Author(s): Qing Chenga, Ying-Ming Jia, Fei-Hu Cheng and Xin-Hua Liu

Volume 11 , Issue 5 , 2014

Page: [572 - 577] Pages: 6

DOI: 10.2174/1570180810666131122234935

Price: $65

Abstract

A series of novel 4-bromo-2-(3-methyl-1-(substituted-phenylsulfonyl)-4,5-dihydro-1H-pyrazol-5-yl) phenol derivatives were synthesized and characterized by NMR, ESI-MS. Compound 3c was determined by X-ray. Biological activity tests results show that compound 3h displayed activity with MIC of 0.39, 0.78, 1.562 µg/mL against B. subtilis ATCC 6633, S. aureus ATCC 6538, P. fluorescens ATCC 13525 and could strongly inhibit S. aureus DNA gyrase and B. subtilis DNA gyrase with IC50s of 0.25 and 0.18 µg/mL respectively.

Keywords: Synthesis, Design, Phenylsulfonyl, Dihydropyrazole, DNA gyrase, Antibacterial activity.


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