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Bioorg Med Chem Lett ; 22(5): 1917-21, 2012 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-22325950

RESUMO

The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacteriumtuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial activity. As part of our research program and with a aim of identifying new antitubercular drug candidates, a new class of 2-(trifluoromethyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazole derivatives has been synthesized by both conventional as well as microwave assisted method and evaluated for their in vitro antitubercular activity against M. tuberculosis H(37)Rv. Moreover, various drug-likeness properties of new compounds were predicted. Seven compounds from the series exhibited good activity with MIC in range 3.12-1.56µg/ml. The present study suggests that compounds 6b, 6c, 6d, 6e and 6f may serve as promising lead scaffolds for further generation of new anti-TB agents.


Assuntos
Antituberculosos/química , Antituberculosos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Rodanina/química , Rodanina/farmacologia , Tiadiazóis/química , Tiadiazóis/farmacologia , Acetatos/síntese química , Acetatos/química , Acetatos/farmacologia , Antituberculosos/síntese química , Humanos , Imidazóis/síntese química , Imidazóis/química , Imidazóis/farmacologia , Testes de Sensibilidade Microbiana , Rodanina/síntese química , Tiadiazóis/síntese química , Tuberculose/tratamento farmacológico
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