Searching for New Cures for Tuberculosis: Design, Synthesis, and Biological Evaluation of 2-Methylbenzothiazoles

摘要: The actual development and clinical use of new therapeutics for tuberculosis (TB) have remained stagnant years because the complexity disease process, treatment which at present requires administration drug combinations over a 6 month period. There is thus an urgent need discovery novel, more active, less toxic anti-TB agents. In this study, we report on chemistry biology series potent 5-(2-methylbenzothiazol-5-yloxymethyl)isoxazole-3-carboxamide derivatives, proved to be active against replicating Mycobacterium (Mtb) H37Rv. most compounds 7j 7s were found inhibit Mtb growth micromolar concentrations, with MIC values 1.4 1.9 μM, respectively. Impressively, all nontoxic toward Vero cells (IC50 > 128 μM). Moreover, best these also tested protozoan parasites, some show activity, especially Pla...