设计、合成及新型（E）-4-氧代-巴豆酰胺衍生物类化合物作为潜在抗结核药物的生物评价。
Design, synthesis, and bioevaluation of a novel class of (E)-4-oxo-crotonamide derivatives as potent antituberculosis agents.
机构信息
Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China.
Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China; Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Beijing Tuberculosis and Thoracic Tumor Research Institute and Beijing Chest Hospital, Capital Medical University, Beijing, China.
出版信息
Bioorg Med Chem Lett. 2019 Feb 15;29(4):539-543. doi: 10.1016/j.bmcl.2019.01.001. Epub 2019 Jan 3.
A series of novel (E)-4-oxo-2-crotonamide derivatives were designed and synthesized to find potent antituberculosis agents. All the target compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis HRv(MTB). Results reveal that 4-phenyl moiety at part A and short methyl group at part C were found to be favorable. Most of the derivatives displayed promising activity against MTB with MIC ranging from 0.125 to 4 µg/mL. Especially, compound IIIa16 was found to have the best activity with MIC of 0.125 μg/mL against MTB and with MIC in the range of 0.05-0.48 µg/mL against drug-resistant clinical MTB isolates.
设计并合成了一系列新型（E）-4-氧代-2-丁烯酰胺衍生物，以寻找有效的抗结核药物。所有目标化合物都进行了体外抗结核分枝杆菌 HRv（MTB）活性评价。结果表明，A 部分的 4-苯基部分和 C 部分的短甲基部分是有利的。大多数衍生物对 MTB 显示出有希望的活性，MIC 范围为 0.125 至 4μg/mL。特别是，化合物 IIIa16 显示出最好的活性，对 MTB 的 MIC 为 0.125μg/mL，对耐药性临床 MTB 分离株的 MIC 范围为 0.05-0.48μg/mL。
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