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Home / Archives for Paulo A

Meta-evaluation of the I Plano Estratégico de Cooperação em Saúde da CPLP (PECS I/CPLP, 2009-2012) with a perspective vision of the II Plano Estratégico de Cooperação em Saúde da CPLP (PECS II/ CPLP 2014-2016)

  • Autores: Craveiro I, Dias S, Hartz Z, Paulo A
  • Ano de Publicação: 2016
  • Journal: Anais do Instituto de Higiene e Medicina Tropical
  • Link: http://ihmtweb.ihmt.unl.pt/PublicacoesFB/Anais/Anais2016-suplemento/index.html#5/z

The first Strategic Plan in Health Cooperation of CPLP (PECS / CPLP) was based on high-level consultation meetings between the Ministries of Health of Member States of CPLP and consists of seven Strategic Axes and their objectives, Priority Projects, operationalization structures, Financing and Execution of Projects. Meta-evaluation was literally defined by Scriven (1969) as the […]
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Bis-alkylamineIndolo[3,2-b]quinolines as hemozoin ligands: implications for antimalarialcytostatic and cytocidal activities

  • Autores: Charneira C, Figueiras M, Gut J, Lavrado J, Lopes D, Machado M, Moreira R, Nogueira F, Paulo A, Rosenthal PJ, Santos SA
  • Ano de Publicação: 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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N10,N11-di-alkylamine indolo[3,2-b]quinolines as hemozoin inhibitors: design, synthesis and antiplasmodial activity

  • Autores: Coelho L, Egan TJ, Figueiras M, Gut J, Lavrado J, Moreira R, Nogueira F, Paulo A, Rosenthal PJ, Santos SA, Wicht KJ
  • Ano de Publicação: 2015
  • Journal: Bioorganic & Medicinal Chemistry
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/25725608

We recently reported that potent N10,O11-bis-alkylamine indolo[3,2-b]quinoline antimalarials act as hemozoin (Hz) growth inhibitors. To improve access and binding to the target we have now designed novel N10,N11-di-alkylamine bioisosteres.
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Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype

  • Autores: Coelho L, Lukens AK, Mazitschek R, Moreira R, Nogueira F, Paulo A, Santos SA, Wirth DF
  • Ano de Publicação: 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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Bis-alkylamine quindolone derivatives as new antimalarial leads

  • Autores: Figueiredo P, Gani K, Gut J, Lavrado J, Lopes D, Moreira R, Nobre PA, Paulo A, Rosário VD, Rosenthal PJ, Santos SA
  • Journal: Bioorganic & Medicinal Chemistry Letters
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Bis-alkylamine+quindolone+derivatives+as+new+antimalarial+leads

Quindolone derivatives, designed to target the malaria parasite digestive vacuole and heme detoxification pathway, have been synthesized by reaction with 2-chloro-N,N-diethylethanamine. This reaction gave N,O-, N,N- and O-alkylated products containing one or two basic side-chains. The compounds were evaluated for antiplasmodial activity against the chloroquine-resistant Plasmodium falciparum W2 strain and for cytotoxicity in HepG2 A16 […]
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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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