Anti-Mycobacterium tuberculosis activity of naphthoimidazoles combined with isoniazid and rifampicin.

Autor: Corrêa Barros LP; Núcleo de Pesquisa em Microbiologia Médica, Faculdade de Medicina, Universidade Federal do Rio Grande - FURG, Rua General Osório, s/nº, Centro, CEP 96.200-400, Rio Grande, RS, Brazil. Electronic address: lelia@vetorialnet.com.br., Del Rio KP; Instituto de Pesquisas em Produtos Naturais, Centro de Ciências da Saúde, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address: karina.p.delrio@gmail.com., Carvalho TDSC; Instituto de Pesquisas em Produtos Naturais, Centro de Ciências da Saúde, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address: thathiane.carvalho@gmail.com., Pinto MDCFR; Instituto de Pesquisas em Produtos Naturais, Centro de Ciências da Saúde, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address: freirecarmo@yahoo.com.br., de Moura KCG; Instituto de Pesquisas em Produtos Naturais, Centro de Ciências da Saúde, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address: kelly.gallan@gmail.com., Halicki PCB; Núcleo de Pesquisa em Microbiologia Médica, Faculdade de Medicina, Universidade Federal do Rio Grande - FURG, Rua General Osório, s/nº, Centro, CEP 96.200-400, Rio Grande, RS, Brazil. Electronic address: priscilahalicki@hotmail.com., Ramos DF; Núcleo de Pesquisa em Microbiologia Médica, Faculdade de Medicina, Universidade Federal do Rio Grande - FURG, Rua General Osório, s/nº, Centro, CEP 96.200-400, Rio Grande, RS, Brazil. Electronic address: daniferamos@gmail.com., da Silva PEA; Núcleo de Pesquisa em Microbiologia Médica, Faculdade de Medicina, Universidade Federal do Rio Grande - FURG, Rua General Osório, s/nº, Centro, CEP 96.200-400, Rio Grande, RS, Brazil. Electronic address: pedrefurg@gmail.com.
Jazyk: angličtina
Zdroj: Tuberculosis (Edinburgh, Scotland) [Tuberculosis (Edinb)] 2018 Jul; Vol. 111, pp. 198-201. Date of Electronic Publication: 2018 Jul 03.
DOI: 10.1016/j.tube.2018.06.015
Abstrakt: Tuberculosis (TB) is the cause of more than one million deaths worldwide, and despite being a curable disease, some factors can make therapy difficult, emphasizing the need for the development of new drugs that may potentiate the action of the classic anti-TB antimicrobials. Naphthoimidazoles show a broad spectrum of biological activities, including antimycobacterial activity. The aim of this study was to evaluate the anti-Mycobacterium tuberculosis activity of nine naphthoimidazoles, alone and combined with isoniazid (INH) and rifampicin (RIF). We evaluated the minimum inhibitory concentration (MIC) of the compounds, the fractional inhibitory concentration of the combinations of the naphthoimidazoles with INH or RIF, and the cytotoxicity of these compounds. Eight compounds showed MICs ranging from 1.56 to 25 μg/mL and the presence of substituents on phenyl groups shown to be essential for antimycobacterial activity. Four compounds showed additivity with both INH and RIF and showed SI values higher than 10, indicating safety. Thus, considering the antimycobacterial activity and the absence of antagonism between naphthoimidazoles and the two main drugs for TB treatment, these compounds could be scaffolds for the development of new anti-TB drugs.
(Copyright © 2018. Published by Elsevier Ltd.)
Databáze: MEDLINE
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