Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives

A series of novel 1,3-dimethylisocyanurates has been synthesized as potential inhibitors of β-ketoacyl synthase in mycobacteria. Most of the 25 compounds described and tested for their activity against M. tuberculosis have a bacteriostatic effect, comparable and even higher that of first-line antituberculosis drugs. These compounds are nontoxic, species-specific, exhibiting no activity against other bacterial species. Synthesis of isocyanurates with anti-TB activity. [Display omitted] ► New anti-TB compounds containing isocyanurate fragment have been synthesized. ► These compounds are potential inhibitors of β-ketoacyl synthase in mycobacteria. ► They have good activity against M. Tuberculosis (MIC 0.05–25 μg/mL). ► These compounds are nontoxic and highly species-specific. ► The efficacy varies with alkyl spacer length and combination of functional groups.