Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
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, Xin-Hua Liu.

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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Article Details

VOLUME: 11
ISSUE: 5
Year: 2014
Page: [572 - 577]
Pages: 6
DOI: 10.2174/1570180810666131122234935
Price: $58