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Synthesis and anti-tubercular activity of a series of 2-sulfonamido/trifluoromethyl-6-substituted imidazo-[2, 1-b]-1, 3, 4-thiadiazole derivatives
Bioorganic and medicinal chemistry ; 12(21): 5651-5659, July, 2004. ilustab
Artigo em Inglês | MedCarib | ID: med-17553
Biblioteca responsável: TT5
A series of 2-sulfonamido/trifluoromethyl-6-(40-substituted aryl/heteroaryl)imidazo[2,1-b]-1,3,4-thiadiazole derivatives(II) have been synthesized by reaction of 2-amino-5-sulfonamido/trifluoromethyl-1,3,4-thiadiazoles and an appropriate a-haloaryl/heteroaryl ketones. Further 5-bromo (III), 5-thiocyanato (IV), 5-gaunylhydrazone (V) derivatives were synthesized in order to study the effect of these substituents on biological activity. Structures of these compounds were established by IR, 1H NMR,13C NMR, Mass and HRMS. The selected compounds were evaluated for their preliminary in vitro anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv strain using radiometric BACTEC and broth dilution assay methods. The results show that compounds 5, 7, 8, 10 and 12 exhibited moderate to good anti-tubercular activity with percentage inhibition of 29, 43, 58, 31and 41, respectively, at a MIC of > 6.25lg/mL. Compound 18 showed a MIC of 20lg/mL.





Coleções: Bases de dados internacionais Base de dados: MedCarib Assunto principal: Sulfonamidas / Tiadiazóis Limite: Humanos Idioma: Inglês Revista: Bioorganic and medicinal chemistry Ano de publicação: 2004 Tipo de documento: Artigo Instituição/País de afiliação: JN Medical College/India