Marchand P., Bazin M. A., Pagniez F., Riviere G., Bodero L., Marhadour S., Nourrisson M. R., Picot C., Ruchaud S., Bach S., Baratte B., Sauvain Michel, Pareja D. C., Vaisberg A. J., Le Pape P. (2015). Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines. European Journal of Medicinal Chemistry, 103, p. 381-395. ISSN 0223-5234.
Titre du document
Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines
Année de publication
2015
Auteurs
Marchand P., Bazin M. A., Pagniez F., Riviere G., Bodero L., Marhadour S., Nourrisson M. R., Picot C., Ruchaud S., Bach S., Baratte B., Sauvain Michel, Pareja D. C., Vaisberg A. J., Le Pape P.
Source
European Journal of Medicinal Chemistry, 2015,
103, p. 381-395 ISSN 0223-5234
A series of original 2-phenyl-3-(pyridin-4-yl)imidazo[1,2-a]pyrazines and the 3-iodo precursors, bearing a polar moiety at the C-8 position, was synthesized and evaluated for their antileishmanial activities. Two derivatives exhibited very good activity against the promastigote and the amastigote forms of Leishmania major in the micromolar to submicromolar ranges, coupled with a low cytotoxicity against macrophages and 3T3 mouse fibroblast cells. Through LmCK1 inhibition assay, investigations of the putative molecular target of these promising antileishmanial compounds will be discussed.
Plan de classement
Sciences fondamentales / Techniques d'analyse et de recherche [020]
;
Entomologie médicale / Parasitologie / Virologie [052]
Localisation
Fonds IRD [F B010065400]
Identifiant IRD
fdi:010065400
