抗细菌
异烟肼
代谢稳定性
化学
肺结核
组合化学
药品
结核分枝杆菌
药理学
立体化学
生物
医学
体外
生物化学
病理
作者
Estêvão Silveira Grams,Alessandro Silva Ramos,Mauro Neves Muniz,Raoní Scheibler Rambo,Marcia Alberton Perelló,Nathalia Denise de Moura Sperotto,Laura Calle González,Lovaine Silva Duarte,Luiza Galina,Adilio Silva Dadda,Guilherme Arraché Gonçalves,Cristiano Valim Bizarro,Luiz Augusto Basso,Pablo Machado
出处
期刊:Molecules
[MDPI AG]
日期:2022-04-15
卷期号:27 (8): 2556-2556
被引量:1
标识
DOI:10.3390/molecules27082556
摘要
Tuberculosis remains a global health problem that affects millions of people around the world. Despite recent efforts in drug development, new alternatives are required. Herein, a series of 27 N-(4-(benzyloxy)benzyl)-4-aminoquinolines were synthesized and evaluated for their ability to inhibit the M. tuberculosis H37Rv strain. Two of these compounds exhibited minimal inhibitory concentrations (MICs) similar to the first-line drug isoniazid. In addition, these hit compounds were selective for the bacillus with no significant change in viability of Vero and HepG2 cells. Finally, chemical stability, permeability and metabolic stability were also evaluated. The obtained data show that the molecular hits can be optimized aiming at the development of drug candidates for tuberculosis treatment.
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