5-硝基-2,6-二氧代六氢-4-嘧啶甲酰胺：合成、体外抗分枝杆菌活性、细胞毒性和异柠檬酸裂解酶抑制研究。
5-Nitro-2,6-dioxohexahydro-4-pyrimidinecarboxamides: synthesis, in vitro antimycobacterial activity, cytotoxicity, and isocitrate lyase inhibition studies.
机构信息
Medicinal Chemistry & Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad, Andhra Pradesh, India.
出版信息
J Enzyme Inhib Med Chem. 2010 Dec;25(6):765-72. doi: 10.3109/14756360903425221. Epub 2010 Jun 23.
Fourteen 5-nitro-2,6-dioxohexahydro-4-pyrimidinecarboxamides (3a-n) were synthesized and evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv (MTB), multidrug-resistant Mycobacterium tuberculosis (MDR-TB), and Mycobacterium smegmatis (MC(2)), as well as their cytotoxicity and MTB isocitrate lyase (ICL) inhibition activity. 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-methyl)-4-[(5-nitro-2,6-dioxohexahydro-4-pyrimidinyl)carbonyl]piperazino-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid (3n) was found to be the most active compound in vitro with MICs of < 0.17 and 0.17 μM against log-phase MTB and MDR-TB, respectively. Some compounds showed 20-45% inhibition against MTB ICL at 10 μM.
合成了 14 种 5-硝基-2,6-二氧代六氢-4-嘧啶甲酰胺（3a-n），并评估了它们对结核分枝杆菌 H37Rv（MTB）、耐多药结核分枝杆菌（MDR-TB）和耻垢分枝杆菌（MC（2））的体外活性，以及它们的细胞毒性和 MTB 异柠檬酸裂解酶（ICL）抑制活性。发现 1-环丙基-6-氟-8-甲氧基-7-[3-甲基]-4-[(5-硝基-2,6-二氧代六氢-4-嘧啶基)羰基]哌嗪-4-氧代-1,4-二氢-3-喹啉羧酸（3n）是体外最有效的化合物，对对数期 MTB 和 MDR-TB 的 MIC 分别为<0.17 和 0.17 μM。一些化合物在 10 μM 时对 MTB ICL 的抑制率为 20-45%。
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