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Synthesis and evaluation of anti-tubercular and antibacterial activities of new 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives. Part 2

2012; Elsevier BV; Volume: 49; Linguagem: Inglês

10.1016/j.ejmech.2012.01.007

1768-3254

Xiaoyun Lu, Xiaobo Liu, Baojie Wan, Scott G. Franzblau, Lili Chen, Changlin Zhou, Qidong You,

Click Chemistry and Applications

A series of substituted 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives were synthesized. The derivatives were screened for in vitro anti-tubercular activities against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA), and antibacterial activities with agar dilution method against clinical S. aureus, E. coli, S. pneumoniae and penicilin-resistant S. pneumoniae. Among 15 compounds, several thiazole derivatives exhibited good anti-tubercular activities with MIC values between 1 μM and 61.2 μM, and potent activities against S. pneumoniae with MIC values less than 0.134 μM. These studies suggest that the thiazole scaffold may serve as a new promising template for further elaboration as anti-tubercular and antibacterial drugs.