5-硝基-2-糠酸腙类化合物的设计、合成及对对数期和饥饿期分枝杆菌体外抗分枝杆菌活性评价
5-Nitro-2-furoic acid hydrazones: design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures.
机构信息
Medicinal Chemistry & Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Andhra Pradesh, India.
出版信息
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4313-6. doi: 10.1016/j.bmcl.2010.06.096. Epub 2010 Jun 20.
Various 5-nitro-2-furoic acid hydrazones were synthesized and evaluated for in vitro activities against log and starved phase culture of two mycobacterial species and Mycobacterium tuberculosis (MTB) isocitrate lyase (ICL) enzyme inhibition studies. Among twenty one compounds, 5-nitro-N'-[(5-nitro-2-furyl)methylidene]-2-furohydrazide (4o) was found to be the most active compound in vitro with MICs of 2.65 and 10.64 microM against log- and starved-phase culture of MTB. Compound 4o also showed good enzyme inhibition of MTB ICL at 10 microM. The docking studies also confirmed the binding potential of the compounds at the ICL active site.
合成了各种 5-硝基-2-糠酸腙，并评估了它们对两种分枝杆菌物种的对数期和饥饿期培养物以及结核分枝杆菌（MTB）异柠檬酸裂解酶（ICL）的体外活性抑制研究。在 21 种化合物中，5-硝基-N'-[(5-硝基-2-呋喃基)亚甲基]-2-糠酰肼（4o）被发现是最具活性的化合物，对 MTB 的对数期和饥饿期培养物的 MIC 分别为 2.65 和 10.64 μM。化合物 4o 对 10 μM 的 MTB ICL 也显示出良好的酶抑制作用。对接研究也证实了化合物在 ICL 活性部位的结合潜力。
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