In:
Letters in Drug Design & Discovery, Bentham Science Publishers Ltd., Vol. 20, No. 11 ( 2023-11), p. 1861-1866
Abstract:
Many contagious diseases have been caused by a variety of nontuberculous mycobacteria,
opportunistic pathogens that can cause disseminated or localized diseases, particularly pulmonary, skin, and soft tissue infections. Objective: In this study fifty-five substituted 4-N-alkylated-2-trifluoromethylquinolines were evaluated
against five species of nontuberculous mycobacteria: Mycobacterium fortuitum, Mycobacterium chelonae, Mycobacterium abscessus, Mycobacterium kansasii, and Mycobacterium avium. Methods: The antimycobacterial activities of all tested compounds were assessed using the microplate
procedure with broth microdilution assay. The most actives were selected for their potential cytotoxic activity against Vero cells. Results: Most of the compounds displayed some activity against M. kansaii, of which 12, 15, 34, 37 and
48 were the most active at 3.12 μg/mL. The derivative 8 was the most active against M. fortuitum at 6.25 μg/mL and the most active against M. chelonae at 3.12 μg/mL. The derivative 2 was the most active
against M. avium at 12.5 μg/mL, and 9 the most active against M. abscessus at 12.5 μg/mL. All the most active compounds showed MIC values similar to the references drugs used against these species. Conclusion: 47 compounds displayed some activity against some of the species analyzed, highlighting
derivatives 12, 15, 34, 37, and 48, which presented the lower MIC values. Compounds 34 and 37 displayed the highest activity and did not show cytotoxicity against Vero cells. These findings have opened
new perspectives for the research of new drugs against these mycobacterial species based on the quinoline nucleus.
Type of Medium:
Online Resource
ISSN:
1570-1808
DOI:
10.2174/1570180819666220704113825
Language:
English
Publisher:
Bentham Science Publishers Ltd.
Publication Date:
2023
SSG:
15,3
Bookmarklink