ienz_a_1101094_sm8562.pdf (2.43 MB)
Library of diversely substituted 2-(quinolin-4-yl)imidazolines delivers novel non-cytotoxic antitubercular leads
journal contribution
posted on 2015-10-30, 00:00 authored by Mikhail Krasavin, Prashant Mujumdar, Vladislav Parchinsky, Tatiana Vinogradova, Olga Manicheva, Marine DogonadzeA novel library based on quinolin-4-ylimidazoline core was designed to incorporate a general quinoline antimicrobial pharmacophore. A synthesis of the well-characterized library of 36 compounds was achieved using the Pd-catalyzed Buchwald–Hartwig-type imidazoline arylation chemistry developed earlier. Compounds were tested for biological activity and were found to possess no antimalarial activity. However, the library delivered two promising antitubercular leads, which are non-cytotoxic and can be further optimized with respect to antimycobacterial potency.