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| MARTINEZ,PABLO D.G.; KRAKE,SUSANN H.; POGGI,MAITIA L.; CAMPBELL,SIMON F.; WILLIS,PAUL A.; DIAS,LUIZ C.. |
| ABSTRACT Combination therapy drugs are considered a fundamental way to control malaria as it mimimizes the risk of emergence of resistance to the individual partner drugs. Consequently, this type of therapy constitutes a driving force for the discovery of new drugs with different modes of action, since this will provide options for combining different drugs to achieve the optimum antimalarial treatment. In this context, a 2,3,8-trisubstitued quinoline compound was found in a high throughput screen (HTS) to show an excellent inhibition of P. falciparum NF54 (IC50 = 22 nM) and low cytotoxicity. We performed a detailed evaluation of the substituents to improve the metabolic stability and solubility liabilities of the original hit and identified derivatives... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Antimalarial activity; Trisubstituted quinoline; SAR; Resistance. |
| Ano: 2018 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652018000301215 |
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| Dolabela,Maria Fâni; Oliveira,Salma G.; Peres,José M.; Nascimento,José M.S.; Póvoa,Marinete M.; Oliveira,Alaide B.. |
| Ethnomedicinal informations point to some Aspidosperma species (Apocynaceae) as antimalarial plants in Brazil and have motivated the evaluation of six species which were collected in the state of Minas Gerais: A. cylindrocarpon Müll. Arg., A. parvifolium A. DC., A. olivaceum Müll. Arg., A. ramiflorum Müll. Arg., A. spruceanum Benth. ex Müll. Arg. and A. tomentosum Mart.. A total of 23 extracts of different plant parts in different solvents were assayed in vitro against chloroquine-resistant (W2) and chloroquine-sensitive (3D7) strains of Plasmodium falciparum. All the extracts were shown to be active with IC50 values in the range of 5.0 ± 0 2.8 µg/mL to 65.0 ± 4.2 µg/mL. TLC profile of the extracts revealed the presence of alkaloids in the six species... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Antimalarial activity; Plasmodium falciparum; In vitro assays; Aspidosperma spp.; Apocynaceae. |
| Ano: 2012 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652012000400005 |
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| Campos, Pierre-eric; Pichon, Emmanuel; Moriou, Céline; Clerc, Patricia; Trépos, Rozenn; Frederich, Michel; De Voogd, Nicole; Hellio, Claire; Gauvin-bialecki, Anne; Al-mourabit, Ali. |
| Chemical study of the CH2Cl2-MeOH (1:1) extract of the sponge Fascaplysinopsis reticulata collected in Mayotte highlighted three new tryptophan derived alkaloids, 6,6′-bis-(debromo)-gelliusine F (1), 6-bromo-8,1′-dihydro-isoplysin A (2) and 5,6-dibromo-8,1′-dihydro-isoplysin A (3), along with the synthetically known 8-oxo-tryptamine (4) and the three known molecules from the same family, tryptamine (5), (E)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (6) and (Z)-6-bromo-2′-demethyl-3′-N-methylaplysinopsin (7). Their structures were elucidated by 1D and 2D NMR spectra and HRESIMS data. All compounds were evaluated for their antimicrobial and their antiplasmodial activities. Regarding antimicrobial activities, the best compounds are (2) and (3), with minimum... |
| Tipo: Text |
Palavras-chave: Fascaplysinopsis reticulata; Marine sponge; Tryptamine alkaloids; Antimalarial activity; Antimicrobial activity. |
| Ano: 2019 |
URL: https://archimer.ifremer.fr/doc/00485/59664/62722.pdf |
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