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Home / Archives for Bioorganic & Medicinal Chemistry

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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Selective hydroboration of dieneamines. Formation of hydroxyalkylphenothiazines as MDR modulators.

  • Autores: Amaral L, Bombicz P, Egyed O, Hajos G, Jemnitz K, Molnar J, Nagy I, Riedl Z, Takács D
  • Journal: Bioorganic & Medicinal Chemistry
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Selective+hydroboration+of+dieneamines.+Formation+of+hydroxyalkylphenothiazines+as+MDR+modulators

N-dienylphenothiazines synthesized from tetrazolo[1,5-a]pyridinium salts by treatment with phenothiazine were subjected to catalytic hydrogenation to yield N-butylphenothiazines, whereas transformation of these dienes with borane dimethyl sulfide (BH(3) × Me(2)S) resulted in selective hydroboration of one double bond and full reduction of the other double bond to give 2-hydroxybutylphenothiazines. Position of the hydroxyl group was supported by NMR spectroscopy and verified by X-ray analysis. Comparison of MDR modulatory activity of the new derivatives revealed that the hydroxybutyl compounds are promising candidates for development of novel MDR inhibitors.
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Karavilagenin C derivatives as antimalarials.

  • Autores: Ferreira MJ, Lopes D, Molnar J, Mulhovo S, Ramalhete C, Rosário VE
  • Journal: Bioorganic & Medicinal Chemistry
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Karavilagenin+C+derivatives+as+antimalarials

Karavilagenin C (1), a cucurbitane-type triterpenoid, previously isolated from the aerial parts of Momordica balsamina, was acylated with different alkanoyl, aroyl and cinnamoyl chlorides/anydrides, yielding ten new mono or diesters, karavoates F (7) and H-P (8-16).
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Triterpenoids as inhibitors of erythrocytic and liver stages of Plasmodium infections.

  • Autores: da Cruz FP, Ferreira MJ, Lopes D, Mulhovo S, Prudencio M, Ramalhete C, Rosário VE
  • Journal: Bioorganic & Medicinal Chemistry
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Triterpenoids+as+inhibitors+of+erythrocytic+and+liver+stages+of+Plasmodium+infections

Bioassay-guided fractionation of the methanol extract of Momordica balsamina led to the isolation of two new cucurbitane-type triterpenoids, balsaminol F (1) and balsaminoside B (2), along with the known glycosylated cucurbitacins, cucurbita-5,24-diene-3β,23(R)-diol-7-O-β-D-glucopyranoside (3) and kuguaglycoside A (4). Compound 1 was acylated yielding two new triesters, triacetylbalsaminol F (5) and tribenzoylbalsaminol F (6).
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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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