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Home / Archives for European Journal of Medicinal Chemistry

Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium

  • Autores: Barreca ML, Cannalire R, Cecchetti V, Couto I, Felicetti T, Machado D, Manfroni G, Massari S, Sabatini S, Santos Costa S, Tabarrini O, Viveiros M
  • Ano de Publicação: 2017
  • Journal: European Journal of Medicinal Chemistry
  • Link: https://www.ncbi.nlm.nih.gov/pubmed/28964936

Mycobacterium avium is a difficult-to-treat pathogen able to quickly develop drug resistance. Like for other microbial species, overexpression of efflux pumps is one of the main mechanisms in developing multidrug resistance. Although the use of efflux pumps inhibitors (EPIs) represents a promising strategy to reverse resistance, to date few M. avium EPIs are known. Recently, the […]
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Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity

  • Autores: Carrasco MP, dos Santos DJ, Gois A, Gonçalves L, Guedes RC, Gut J, Hänscheid T, Machado M, Moreira R, Newton AS, Nogueira F, Rosenthal PJ
  • Ano de Publicação: 2014
  • Journal: European Journal of Medicinal Chemistry
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/24813880

A library comprising 44 diversely substituted aurones derivatives was synthesized by straightforward aldol condensation reactions of benzofuranones and the appropriately substituted benzaldehydes. Microwave enhanced synthesis using palladium catalyzed protocols was introduced as a powerful strategy for extending the chemical space around the aurone scaffold.
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Design, synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity

  • Autores: Aires-de-Sousa J, Correia HE, Elvas-Leitao R, Kovalishyn V, Latino DARS, Martins F, Miranda V, Ramos J, Reis M, Santos L, Santos S, Ventura C, Vitorino S, Viveiros M
  • Ano de Publicação: 2014
  • Journal: European Journal of Medicinal Chemistry
  • Link: http://www.sciencedirect.com/science/article/pii/S0223523414004061

The disturbing emergence of multidrug-resistant strains of Mycobacterium tuberculosis(Mtb) has been driving the scientific community to urgently search for new and efficient antitubercular drugs. Despite the various drugs currently under evaluation, isoniazid is still the key and most effective component in all multi-therapeutic regimens recommended by the WHO. This paper describes the QSAR-oriented design, synthesis and in vitro antitubercular activity of several potent isoniazid derivatives (isonicotinoyl hydrazones and isonicotinoyl hydrazides) against H37Rv and two resistant Mtb strains.
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Probing the aurone scaffold against Plasmodium falciparum: Design, synthesis and antimalarial activity

  • Autores: Carrasco MP, dos Santos DJVA, Gois A, Gonçalves L, Guedes RC, Gut J, Haenscheid T, Machado M, Moreira R, Newton AS, Nogueira F, Rosenthal PJ
  • Ano de Publicação: 2014
  • Journal: European Journal of Medicinal Chemistry
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/24813880

A library comprising 44 diversely substituted aurones derivatives was synthesized by straightforward aldol condensation reactions of benzofuranones and the appropriately substituted benzaldehydes. Microwave enhanced synthesis using palladium catalyzed protocols was introduced as a powerful strategy for extending the chemical space around the aurone scaffold.
Ler mais

About GHTM

GHTM is a R&D Center that brings together researchers from IHMT 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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