4.7 Article

Synthesis and antitubercular screening of imidazole derivatives

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 8, 页码 3350-3355

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ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.02.013

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Tuberculosis; Imidazoles; Glycosyl amino ester; C-alkylation; C-Allyl imidazoles

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A series of imidazole based compounds were synthesized by reacting simple imidazoles with alkyl halides or alkyl halocarboxylate in presence of tetrabutylammonium bromide (TBAB). The compounds bearing carbethoxy group undergo amidation with different amines in the presence of DBU to give respective carboxamides. The synthesized compounds were screened against Mycobacterium tuberculosis where compound 17 exhibited very good in vitro antitubercular activity and may serve as a lead for further optimization. (C) 2009 Elsevier Masson SAS. All rights reserved.

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