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

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

Volume: 11 Issue: 5

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

Affiliation:

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 IC_50s of 0.25 and 0.18 µg/mL respectively.

Cite this article as:

Chenga Qing, Jia Ying-Ming, Cheng Fei-Hu and Liu Xin-Hua, Novel 4-bromo-2-(3-methyl-1-(substituted-phenylsulfonyl)-4,5-dihydro-1- H-pyrazol-5-yl)phenol Derivatives: Synthesis and Antibacterial Activity, Letters in Drug Design & Discovery 2014; 11 (5) . https://dx.doi.org/10.2174/1570180810666131122234935