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

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.

Graphical abstractA series of thiazole, oxazole and imidazole derivatives were designed, synthesized and evaluated for anti-tubercular and antibacterial activity. Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► A series of substituted thiazole, oxazole and imidazole derivatives were designed and synthesized. ► The derivatives were screened for anti-tubercular and antibacterial activities. ► Several thiazoles exhibited anti-tubercular activities with MIC values of 1–61.2 μM ► Several thiazoles also exhibited potent activities against S. pneumoniae with MIC values less than 0.134 μM.