Lu Xiaoyun, Hu Xianglong, Liu Zhiyong, Zhang Tianyu, Wang Ruibing, Wan Baojie, Franzblau Scott G, You Qidong
School of Pharmacy , Jinan University , 601 Huangpu Avenue West , Guangzhou , 510632 , China . Email:
Jiangsu Key Laboratory of Drug Design and Optimization , China Pharmaceutical University , Nanjing 210009 , China . Email:
Medchemcomm. 2017 Apr 28;8(6):1303-1306. doi: 10.1039/c7md00146k. eCollection 2017 Jun 1.
A series of benzylsulfanyl benzo-heterocycle amides and hydrazones were synthesized and evaluated for anti-tubercular activities. The isonicotinyl hydrazone derivatives , and exhibited good anti-tubercular activity against HRv (ATCC #27294) with MIC values of 0.23, 0.24 and 0.24 μM, respectively, and were also active against SDR-TB, MDR-TB and XDR-TB. More importantly, compound also showed low cytotoxicity and good metabolic stability, and could significantly reduce the mycobacterial burden in a mouse model infected with autoluminescent H37Ra strain, which may serve as a lead compound for further development.
合成了一系列苄硫基苯并杂环酰胺和腙，并对其抗结核活性进行了评估。异烟酰腙衍生物 、 和 对人耐药结核分枝杆菌（HRv，ATCC #27294）表现出良好的抗结核活性，MIC值分别为0.23、0.24和0.24 μM，并且对单耐药结核病、多耐药结核病和广泛耐药结核病也有活性。更重要的是，化合物 还表现出低细胞毒性和良好的代谢稳定性，并且可以显著降低感染自发光H37Ra菌株的小鼠模型中的分枝杆菌负荷，这可能作为进一步开发的先导化合物。
