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Updated: May 29, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Diarylquinolines, synthesis pathways and quantitative structure--activity relationship studies leading to the
Jerome Guillemont1, Christophe Meyer, Alain Poncelet
1Janssen-Cilag France, Campus de Maigremont, BP615, 27106, Val de Reuil Cedex, France. jguillem@its.jnj.com
Abstract:
The emergence of multidrug-resistant strains of Mycobacterium tuberculosis and resistance to current anti-TB drugs call for the discovery and development of new effective anti-TB drugs. TMC207 is the lead candidate of a novel class of antimycobacterial agents, the diarylquinolines, which specifically inhibit mycobacterial ATP synthase and displays high activity against both drug-susceptible and multidrug-resistant strains of Mycobacterium tuberculosis. This article covers both synthesis pathways as well as qualitative and quantitative analyses of the structure-activity relationships of the diarylquinoline series on Mycobacterium smegmatis activity.
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