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新型3-[3-(取代苯基)-1-异烟酰基-1H-吡唑-5-基]-2H-色烯-2-酮衍生物的合成及其抗菌活性

Synthesis and antibacterial activity of a new series of 3-[3-(substituted phenyl)-1-isonicotinoyl-1H-pyrazol-5-yl]-2H-chromen-2-one derivatives.

作者信息

Aragade Prashant, Maddi Veeresh, Khode Suresh, Palkar Mahesh, Ronad Pradeepkumar, Mamledesai Shivalingarao, Satyanarayana Darbhamulla

机构信息

Department of Pharmaceutical Chemistry, KLES' College of Pharmacy, Vidyanagar, Hubli, Karnataka, India.

出版信息

Arch Pharm (Weinheim). 2009 Jun;342(6):361-6. doi: 10.1002/ardp.200800156.

Abstract

A novel series of 3-[3-(substituted phenyl)-1-isonicotinoyl-1H-pyrazol-5-yl]-2H-chromen-2-one derivatives 4a-k have been synthesized by the reaction of 3-[2,3-dibromo-3-(substituted phenyl) propanoyl]-2H-chromen-2-one 3a-k and isonicotinic acid hydrazide in the presence of triethylamine in absolute ethanol, characterized by spectral data and screened for their in-vitro antibacterial activity against Gram-positive and Gram-negative bacteria. Among the series, compounds 4e, 4i, and 4k displayed an encouraging antibacterial activity profile as compared to the reference drug ampicillin against tested bacterial strains.

摘要

通过3-[2,3-二溴-3-(取代苯基)丙酰基]-2H-色烯-2-酮3a-k与异烟肼在三乙胺存在下于无水乙醇中反应,合成了一系列新型的3-[3-(取代苯基)-1-异烟酰基-1H-吡唑-5-基]-2H-色烯-2-酮衍生物4a-k,通过光谱数据对其进行了表征,并对它们针对革兰氏阳性和革兰氏阴性细菌的体外抗菌活性进行了筛选。在该系列中,与参比药物氨苄西林相比,化合物4e、4i和4k对受试菌株显示出令人鼓舞的抗菌活性。

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