Synthesis of Potential Inhibitors of InhA with Pyrrolidine-2,5-dione Core Fragment and Evaluation of their Biological Activity

Matviiuk, T., Gorichko, M., Lherbet, C., Rodriguez, F., Baltas, M., Rosalia Pasca, M., Voitenko, Z. (2013). Synthesis of Potential Inhibitors of InhA with Pyrrolidine-2,5-dione Core Fragment and Evaluation of their Biological Activity. French-Ukrainian Journal of Chemistry, 1(1), 15–22.

We report here the discovery, synthesis and screening results of the series of 3-bulky substituted pyrrolidine-2,5-dione derivatives as a novel class of potential inhibitors on InhA, a key enzyme involved in the fatty acid biosynthesis pathway (type II) of M. tuberculosis as well as inhibitors of Mycobacterium tuberculosis H37Rv.