Anti-tubercular Activity of Novel 4-anilinoquinolines and 4-anilinoquinazolines

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2019 Aug 6

PMID 31378571

Citations 8

Authors

Christopher R M Asquith

Neil Fleck

Chad D Torrice

Daniel J Crona

Christoph Grundner

William J Zuercher

Affiliations

Soon will be listed here.

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 MIC 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.

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