Maether M. P., Desoubzdanne D., Izquierdo A., Guieu V., Maturano M., Andre-Barres C., Valentin A., Jullian Valérie, Chevalley Séverine, Maynadier M., Vial H., Payrastre C. (2009). Synthesis and antimalarial properties of streptocyanine dyes. Chemmedchem, 4 (8), p. 1327-1332. ISSN 1860-7179.
Titre du document
Synthesis and antimalarial properties of streptocyanine dyes
Maether M. P., Desoubzdanne D., Izquierdo A., Guieu V., Maturano M., Andre-Barres C., Valentin A., Jullian Valérie, Chevalley Séverine, Maynadier M., Vial H., Payrastre C.
Source
Chemmedchem, 2009,
4 (8), p. 1327-1332 ISSN 1860-7179
Several streptocyanine dyes were synthesized that contain polymethine chains of varying length. Their in vitro antimalarial activities were evaluated against the virulent P. falciparum parasite. In addition to the influence of polymethine chain length, the effects of structural modifications at nitrogen end groups, para substitution of the phenyl groups, and counter-anions were studied. The most potent antimalarial activities were found for heptacarbon chain streptocyanines, with an IC50 value of 60 nM. Interestingly, most of the compounds were less cytotoxic toward the mammalian cells tested. The best selective toxicity profiles were found for pentacarbon chain streptocyanines, which have a good in vitro specificity index.
Plan de classement
Entomologie médicale / Parasitologie / Virologie [052]
;
Sciences du monde végétal [076]
