Adjuvant therapies against tuberculosis: Discovery of a 2-aminothiazole targeting Mycobacterium tuberculosis energetics

Authors: Machado D, Azzali E, Couto I, Costantino G, Pieroni M, Viveiros M
Publication Year: 2018
Journal: Future Microbiology
Link: https://www.futuremedicine.com/doi/10.2217/fmb-2018-0110

AIM: To evaluate the activity of the 2-aminothiazole UPAR-174 following an unexplored approach: targeting Mycobacterium tuberculosis with lipophilic compounds that present antituberculosis and efflux inhibitory activity. METHODS: Antituberculosis activity was assessed against replicating, nonreplicating and intracellular bacilli. Its capacity to inhibit active efflux was determined. ATP quantification and membrane potential analysis were performed. Intracellular activity […]
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Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery

Authors: Azzali E, Cabassi CS, Costantino G, Flisi S, Kaushik A, Lamichhane G, Machado D, Pieroni M, Vacondio F, Viveiros M
Publication Year: 2017
Journal: Journal of Medicinal Chemistry
Link: https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b00793

Tuberculosis remains one of the deadliest infectious diseases in the world, and the increased number of multidrug-resistant and extremely drug-resistant strains is a significant reason for concern. This makes the discovery of novel antitubercular agents a cogent priority. We have previously addressed this need by reporting a series of substituted 2-aminothiazoles capable to inhibit the […]
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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 […]
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Adjuvant therapies against tuberculosis: Discovery of a 2-aminothiazole targeting Mycobacterium tuberculosis energetics

Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery

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

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