5-硝基噻唑衍生物的开发：鉴定针对复制和潜伏结核分枝杆菌的先导化合物。
Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis.
机构信息
Antitubercular Drug Discovery Laboratory, Department of Pharmacy, Birla Institute of Technology& Science - Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India.
出版信息
Bioorg Med Chem Lett. 2012 Dec 15;22(24):7414-7. doi: 10.1016/j.bmcl.2012.10.060. Epub 2012 Oct 23.
Twenty eight 5-nitrothiazole derivatives were synthesized and evaluated for in vitro activities against Mycobacterium tuberculosis (MTB), cytotoxicity against HEK 293T. Among the compounds, 5-nitro-N-(5-nitrothiazol-2-yl)furan-2-carboxamide (20) was found to be the most active compound in vitro with MICs of 5.48 μM against log-phase culture of MTB and also non-toxic up to 100 μM.
合成了 28 种 5-硝基噻唑衍生物，并评估了它们对结核分枝杆菌（MTB）的体外活性和对 HEK 293T 的细胞毒性。在这些化合物中，5-硝基-N-（5-硝基噻唑-2-基）呋喃-2-甲酰胺（20）被发现是体外最具活性的化合物，对对数生长期 MTB 的 MIC 值为 5.48 μM，在高达 100 μM 的浓度下也没有毒性。
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