Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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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

Affiliation: School of Pharmacy, Anhui Medical University, Hefei, 230032, P. R. China.

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

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.

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Article Details

VOLUME: 11
ISSUE: 5
Page: [572 - 577]
Pages: 6
DOI: 10.2174/1570180810666131122234935