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Home / Archives for Lavrado J

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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N10,N11-di-alkylamine indolo[3,2-b]quinolines as hemozoin inhibitors: design, synthesis and antiplasmodial activity

  • Authors: Coelho L, Egan TJ, Figueiras M, Gut J, Lavrado J, Moreira R, Nogueira F, Paulo A, Rosenthal PJ, Santos SA, Wicht KJ
  • Publication Year: 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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Bis-alkylamine quindolone derivatives as new antimalarial leads

  • Authors: 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 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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