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

Authors :
Sophie Marhadour
Olivier Lozach
Laurent Meijer
Patrice Le Pape
Sandrine Ruchaud
Pascal Marchand
Carine Picot
Marc-Antoine Bazin
Fabrice Pagniez
Najma Rachidi
Maud Antoine
Université de Nantes - UFR des Sciences Pharmaceutiques et Biologiques
Université de Nantes (UN)
Cibles et Médicaments des Infections et de l'Immunité (IICiMed)
Nantes Université - UFR des Sciences Pharmaceutiques et Biologiques (Nantes Univ - UFR Pharmacie)
Nantes Université - pôle Santé
Nantes Université (Nantes Univ)-Nantes Université (Nantes Univ)-Nantes Université - pôle Santé
Nantes Université (Nantes Univ)-Nantes Université (Nantes Univ)
Station biologique de Roscoff (SBR)
Sorbonne Université (SU)-Centre National de la Recherche Scientifique (CNRS)
Adaptation et diversité en milieu marin (AD2M)
Station biologique de Roscoff [Roscoff] (SBR)
Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)-Centre National de la Recherche Scientifique (CNRS)
Molécules et cibles thérapeutiques (MCT)
Parasitologie moléculaire et Signalisation
Institut Pasteur [Paris] (IP)-Centre National de la Recherche Scientifique (CNRS)
Centre hospitalier universitaire de Nantes (CHU Nantes)
Source :
European Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, 2012, 58, pp.543-556. ⟨10.1016/j.ejmech.2012.10.048⟩
Publication Year :
2012

Abstract

International audience; 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.

Details

ISSN :
17683254 and 02235234
Volume :
58
Database :
OpenAIRE
Journal :
European journal of medicinal chemistry
Accession number :
edsair.doi.dedup.....544d2ee66881a344587c8c70e60eca4e
Full Text :
https://doi.org/10.1016/j.ejmech.2012.10.048⟩