255833-19-3Relevant academic research and scientific papers
Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant: Mycobacterium tuberculosis
Lu, Xiaoyun,Hu, Xianglong,Liu, Zhiyong,Zhang, Tianyu,Wang, Ruibing,Wan, Baojie,Franzblau, Scott G.,You, Qidong
, p. 1303 - 1306 (2017/07/07)
A series of benzylsulfanyl benzo-heterocycle amides and hydrazones were synthesized and evaluated for anti-tubercular activities. The isonicotinyl hydrazone derivatives 12d, 12e and 12f exhibited good anti-tubercular activity against Mycobacterium tuberculosis H37Rv (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 12e 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.
