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

详细信息    查看全文

• 作者：Sophie Marhadour^a ; Pascal Marchand^a ; ^{pascal.marchand@univ-nantes.fr} ; Fabrice Pagniez^b ; ^{fabrice.pagniez@univ-nantes.fr} ; Marc-Antoine Bazin^a ; Carine Picot^a ; ^b ; Olivier Lozach^c ; Sandrine Ruchaud^c ; Maud Antoine^d ; Laurent Meijer^e ; Najma Rachidi^c ; ^f ; Patrice Le Pape^b
• 关键词：Antileishmanial activity ; 2 ; 3-Diarylimidazo[1 ; 2-a]pyridines ; Direct arylation ; Lipophilicity ; Casein kinase 1
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：December, 2012
• 年：2012
• 卷：58
• 期：Complete
• 页码：543-556
• 全文大小：470 K

文摘

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.