Barres, Sophie

Crepin, Damien

Giraud, Francis

Le Borgne, Marc

Le Pape, Patrice

Logé, Cédric

Pagniez, Fabrice

Picot, Carine

Hal-Diderot

Design, synthesis and evaluation of 3-(imidazol- 1-ylmethyl)indoles as antileishmanial agents. Part II

International audienceA new series of 1-benzyl-3-(imidazol-1-ylmethyl)indoles were synthesized according to a previous 3D-QSAR predictive model and assayed for their antiparasitic activity upon Leishmania mexicana promastigotes. The biological results obtained for these twelve molecules showed an IC50 ranging from 2.3 to 32 μM and mainly illustrated the importance of the hydrophobic parameter the para-position of the benzyl group. In order to improve the activities of these compounds and to check the potential influence of the electronic parameter on this particular position, a Craig diagram was used to select original electro-donating and lipophilic substituents. Synthesis and biological evaluation of ten new compounds (IC50 between 2.5 and 5.4 μM) confirmed that only the hydrophobic field is essential for a high level of activity

Crépin, Damien

HAL: Hyper Article en Ligne

Portail HAL Nantes Université

Olivencia Valdivia, Antonio

Repositorio Institucional de la Universidad de Almería (Spain)