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Home / Archives for Rosenthal PJ

Novel endoperoxide-based transmission-blocking antimalarials with liver- and blood-schizontocidal activities

  • Authors: Albuquerque IS, Amewu R, Capela R, Gut J, Lopes F, Marti F, Meireles P, Miranda D, Moreira R, Mota MM, Nogueira F, O'Neill PM, Oliveira R, Paiva I, Prudencio M, Rosenthal PJ
  • Publication Year: 2013
  • Journal: ACS Medicinal Chemistry Letters
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/24900781

In a search for effective compounds against both the blood- and liver-stages of infection by malaria parasites with the ability to block the transmission of the disease to mosquito vectors, a series of hybrid compounds combining either a 1,2,4-trioxane or 1,2,4,5-tetraoxane and 8-aminoquinoline moieties were synthesized and screened for their antimalarial activity.
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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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Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity

  • Authors: 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
  • Publication Year: 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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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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Novel potent metallocenes against liver stage malaria

  • Authors: Cabrita E, da Cruz FP, Do Rosário VE, Gomes P, Gut J, Matos J, Moreira R, Nogueira F, Prudencio M, Rosenthal PJ
  • Journal: Antimicrobial Agents and Chemotherapy
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Novel+potent+metallocenes+against+liver+stage+malaria.

Novel conjugates of the antimalarial drug primaquine (compound 1) with ferrocene, named primacenes, have been synthesized and screened for their activities against blood stage and liver stage malaria in vitro and host-vector transmission in vivo.
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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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