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[:pb]Antibacterial activity of new substituted 4-N-alkylated-2-trifluoromethyl-quinoline analogues against sensitive and resistant Mycobacterium tuberculosis strains[:]

[:pb]Authors: Da Silva, E. T. ; De Andrade, G. F. ; Araújo, A. S. ; Lourenço, M. C. S. ; De Souza, M. V. N.
Source: European Journal of Pharmaceutical Sciences, v. 157, p. 105596, 2021.
Publisher: ScienceDirect


Abstract

Objectives: The emergence of resistant strain has aggravated the tuberculosis situation in the world, running out
of control and hard to fight. We evaluate forty new quinoline analogues against sensitive and resistant Mycobacterium tuberculosis (Mtb). Methods: The compounds were obtained via synthesis and evaluated against sensitive strain ATCC 27294. Selected compounds were evaluated against resistant strains SR 2571/0215 and T113/09, using the MABA method. The more active compounds were selected for their potential cytotoxic activity against human macrophage cells. Results: Twenty-nine compounds displayed activity against sensitive strain, and thirteen were active against resistant strains. Against sensitive strain, the most promising compounds were 4c and 4d (MIC = 9 and 12 μM, respectively). Against resistant strains, the compounds 4a, 4d displayed the best results (MIC = 4 and 5 μM, respectively). The active compounds 4a, 4d, 6d, 7c, 8d, and 10d were non-cytotoxic to the host cells at concentrations near to the MIC. The non-cytotoxic compound 4d was the most potent against resistant and sensitive Mtb. Conclusion: These findings contribute to relevant information and perspectives in search of new bioactive compounds against sensitive and resistant TB. Resistant strains have turned tuberculosis a severe disease in the world.


Keywords: quinoline, antitubercular, synthesis, drugs, resistant strains
Document Type: Research Article
DOI: 10.1016/j.ejps.2020.105596
Publication date:  1 de fevereiro de 2021[:]

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