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Home / Archives for Journal of Medicinal Chemistry

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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Bis-alkylamineIndolo[3,2-b]quinolines as hemozoin ligands: implications for antimalarialcytostatic and cytocidal activities

  • Authors: Charneira C, Figueiras M, Gut J, Lavrado J, Lopes D, Machado M, Moreira R, Nogueira F, Paulo A, Rosenthal PJ, Santos SA
  • Publication Year: 2014
  • Journal: Journal of Medicinal Chemistry
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/24673163

To get insight into the relevance of targeting hemozoin (Hz) crystals, two isomeric series, N5,N10-bis-alkylamine (2a-k) and N10,O11-bis-alkylamine (3a-k) indolo[3,2-b]quinolines, were evaluated for their in vitro activity against chloroquine (CQ)-resistant and sensitive strains of Plasmodium falciparum.
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Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype

  • Authors: Coelho L, Lukens AK, Mazitschek R, Moreira R, Nogueira F, Paulo A, Santos SA, Wirth DF
  • Publication Year: 2015
  • Journal: Journal of Medicinal Chemistry
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/26295174

A series of 3-piperidin-4-yl-1H-indoles with building block diversity was synthesized based on a hit derived from an HTS whole-cell screen against Plasmodium falciparum. Thirty-eight compounds were obtained following a three-step synthetic approach and evaluated for anti-parasitic activity.
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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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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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