European Journal of Medicinal Chemistry p. 543 - 556 (2012)
Update date:2022-07-30
Topics:
Marhadour, Sophie
Marchand, Pascal
Pagniez, Fabrice
Bazin, Marc-Antoine
Picot, Carine
Lozach, Olivier
Ruchaud, Sandrine
Antoine, Maud
Meijer, Laurent
Rachidi, Najma
Le Pape, Patrice
A novel series of 2,3-diarylimidazo[1,2-a]pyridines was synthesized and evaluated for their antileishmanial activities. Four derivatives exhibited good activity against the promastigote and intracellular amastigote stages of Leishmania major, coupled with a low cytotoxicity against the HeLa human cell line. The impact of compound lipophilicity on antiparasitic activities was investigated by Log D comparison. Although LmCK1 could be the parasitic target for three compounds (13, 18, 21), the inhibition of another target is under study to explain the antileishmanial effect of the most promising compounds.
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Doi:10.1002/ejic.201200368
(2012)Doi:10.1002/adsc.201200235
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