Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.

ID: ALA4385662

Journal: Bioorg Med Chem Lett

Title: Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.

Authors: Asquith CRM, Fleck N, Torrice CD, Crona DJ, Grundner C, Zuercher WJ.

Abstract: We screened a series of 4-anilinoquinolines and 4-anilinoquinazolines and identified novel inhibitors of Mycobacterium tuberculosis (Mtb). The focused 4-anilinoquinoline/quinazoline scaffold arrays yielded compounds with high potency and the identification of 6,7-dimethoxy-N-(4-((4-methylbenzyl)oxy)phenyl)quinolin-4-amine (34) with an MIC₉₀ value of 0.63-1.25 µM. We also defined a series of key structural features, including the benzyloxy aniline and the 6,7-dimethoxy quinoline ring, that are important for Mtb inhibition. Importantly the compounds showed very limited toxicity and scope for further improvement by iterative medicinal chemistry.

CiteXplore: 31378571

DOI: 10.1016/j.bmcl.2019.07.012

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