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Home / Publications / Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy

Rational Design and Synthesis of Thioridazine Analogues as Enhancers of the Antituberculosis Therapy

  • Authors: Azzali E, Costa SS, Costantino G, Couto I, Machado D, Pieroni M, Viveiros M
  • Publication Year: 2015
  • Journal: Journal of Medicinal Chemistry
  • Link: https://pubs.acs.org/doi/10.1021/acs.jmedchem.5b00428

Tuberculosis, caused by Mycobacterium tuberculosis, is still one of the leading infectious diseases globally. Therefore, novel approaches are needed to face this disease. Efflux pumps are known to contribute to the emergence of M. tuberculosis drug resistance. Thioridazine has shown good anti-TB properties both in vitro and in vivo, likely due to its capacity to inhibit efflux mechanisms. Here we report the design and synthesis of a number of putative efflux inhibitors inspired by the structure of thioridazine. Compounds were evaluated for their in vitro and ex vivo activity against M. tuberculosis H37Rv. Compared to the parent molecule, some of the compounds synthesized showed higher efflux inhibitory capacity, less cytotoxicity, and a remarkable synergistic effect with anti-TB drugs both in vitro and in human macrophages, demonstrating their potential to be used as coadjuvants for the treatment of tuberculosis.

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About GHTM

GHTM is a R&D Unit that brings together researchers with a track record in Tropical Medicine and International & Global Health. It aims at strengthening Portugal's role as a leading partner in the development and implementation of a global health research agenda. Our evidence-based interventions contribute to the promotion of equity in health and to improve the health of populations.

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