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

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...

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Detalles Bibliográficos
Autores principales: Grams, Estevão Silveira, Silva Ramos, Alessandro, Neves Muniz, Mauro, Rambo, Raoní S., Alberton Perelló, Marcia, Sperotto, Nathalia, Calle González, Laura, Duarte, Lovaine Silva, Galina, Luiza, Silva Dadda, Adilio, Arraché Gonçalves, Guilherme, Valim Bizarro, Cristiano, Basso, Luiz Augusto, Machado, Pablo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9027910/
https://www.ncbi.nlm.nih.gov/pubmed/35458755
http://dx.doi.org/10.3390/molecules27082556
Descripción
Sumario: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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