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新型苯并咪唑类作为潜在抗菌剂的合成及生物学评价

Synthesis and biological evaluations of novel benzimidazoles as potential antibacterial agents.

作者信息

He Yun, Yang Jun, Wu Baogen, Risen Lisa, Swayze Eric E

机构信息

Ibis Therapeutics, a division of Isis Pharmaceuticals, Inc., 2292 Faraday Avenue, Carlsbad, CA 92008, USA.

出版信息

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1217-20. doi: 10.1016/j.bmcl.2003.12.051.

Abstract

A series of novel benzimidazole derivatives were synthesized via parallel solution-phase chemistry. Many of these compounds were found to inhibit the growth of Staphylococcus aureus and Escherichia coli. Several analogues exhibited low micromolar minimal inhibitory concentrations (MIC) against both Gram-positive and Gram-negative bacteria of clinical relevance and could serve as leads for further optimizations for antibacterial research.

摘要

通过平行溶液相化学合成了一系列新型苯并咪唑衍生物。发现其中许多化合物可抑制金黄色葡萄球菌和大肠杆菌的生长。几种类似物对具有临床相关性的革兰氏阳性和革兰氏阴性细菌均表现出低微摩尔最低抑菌浓度(MIC),可作为抗菌研究进一步优化的先导化合物。

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