含 5 种杂原子取代基的 3- 酰胺基苯酚的设计、合成与抗结核活性。
Design, synthesis, and antitubercular activity of 3-amidophenols with 5-heteroatomic substitutions.
机构信息
Guangdong Provincial Key Laboratory of New Drug Design and Evaluation, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China.
State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Science, Guangzhou, China.
出版信息
Arch Pharm (Weinheim). 2019 Apr;352(4):e1800277. doi: 10.1002/ardp.201800277. Epub 2019 Jan 30.
A series of novel 3-amidophenols with 5-heteroatomic substitutions were designed and synthesized. Several compounds showed potent antitubercular activity against Mycobacterium tuberculosis H37Ra (MIC = 0.25-5 μg/mL). Compounds 12j and 14i also displayed good inhibitory activity against M. tuberculosis H37Rv and two clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.39-3.12 μg/mL). The privileged compound 14i showed certain oral efficacy on a mouse infection model. The compounds are non-cytotoxic against L-O2 hepatocytes and RAW264.7 macrophagocytes. They did not exert inhibitory activity against representative Gram-positive and Gram-negative bacteria.
设计并合成了一系列具有 5 种杂原子取代的新型 3-酰胺基苯酚。几种化合物对结核分枝杆菌 H37Ra 具有很强的抗结核活性（MIC=0.25-5μg/mL）。化合物 12j 和 14i 对结核分枝杆菌 H37Rv 和两种临床分离的耐多药结核分枝杆菌菌株也表现出良好的抑制活性（MIC=0.39-3.12μg/mL）。优势化合物 14i 在小鼠感染模型中显示出一定的口服疗效。这些化合物对 L-O2 肝细胞和 RAW264.7 巨噬细胞没有细胞毒性。它们对代表性的革兰氏阳性和革兰氏阴性细菌没有抑制活性。
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