Alkylated/aminated nitroimidazoles and nitroimidazole-7-chloroquinoline conjugates: Synthesis and anti-mycobacterial evaluation.
Bioorg Med Chem Lett
; 28(8): 1309-1312, 2018 05 01.
Article
em En
| MEDLINE
| ID: mdl-29551480
ABSTRACT
The success in exploring anti-tubercular potency of nitroimidazole and quinoline, the core moieties of recently approved anti-tubercular drugs instigated us to synthesize a series of alkylated/aminated 2-methyl-5-nitroimidazoles and nitroimidazole-7-chloroquinoline conjugates and to evaluate them for their activities against Mycobacterium tuberculosis as well as for their cytotoxicity towards the J774 murine macrophage cell line. Although the synthesized compounds did not surpass the activity of the standard drug Isoniazid, they have appreciable activities with minimal cytotoxicity. The synthesized nitroimidazole-7-chloroquinoline conjugate, 11c, having butyl chain as linker, proved to be the most potent among the series with an MIC50 value of 2.2⯵g/mL.
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Base de dados:
MEDLINE
Assunto principal:
Quinolinas
/
Nitroimidazóis
/
Antituberculosos
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article