Synthesis and Antimycobacterial Evaluation of N-(4-(Benzyloxy)benzyl)-4-aminoquinolines

Molecules

Laura Calle González¹  Pablo Machado¹  Luiza Galina¹  Adilio Silva Dadda¹  Estevão Silveira Grams¹  Luiz Augusto Basso¹  Lovaine Silva Duarte¹  Mauro Neves Muniz¹  Cristiano Valim Bizarro¹  Raoní S. Rambo¹  Marcia Alberton Perelló¹  Guilherme Arraché Gonçalves¹  Alessandro Silva Ramos¹  Nathalia Sperotto¹ 

[1] Instituto Nacional de Ciência e Tecnologia em Tuberculose, Centro de Pesquisas em Biologia Molecular e Funcional, Pontifícia Universidade Católica do Rio Grande do Sul, Porto Alegre 90619-900, RS, Brazil;

关键词: Mycobacterium tuberculosis;    drug discovery;    synthesis;    quinolines;    tuberculosis;   

DOI  :  10.3390/molecules27082556

来源: DOAJ

【 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.

【 授权许可】

Unknown