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© Research
Publication : European journal of medicinal chemistry

Synthesis and biological evaluation of 2,3-diarylimidazo[1,2-a]pyridines as antileishmanial agents.

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in European journal of medicinal chemistry - 02 Nov 2012

Marhadour S, Marchand P, Pagniez F, Bazin MA, Picot C, Lozach O, Ruchaud S, Antoine M, Meijer L, Rachidi N, Le Pape P,

Link to Pubmed [PMID] – 23164660

Link to DOI – 10.1016/j.ejmech.2012.10.048S0223-5234(12)00652-6

Eur J Med Chem 2012 Dec; 58(): 543-56

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.