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

Abstract：

: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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

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

doi

10.1016/j.ejmech.2012.10.048

subject

Has Abstract

pub_date

2012-12-01 00:00:00

pages

543-56

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00652-6

journal_volume

58

pub_type

杂志文章

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