title: 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.
authors.affiliation: Université de Nantes, Nantes Atlantique Universités, Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections et du Cancer, IICiMed UPRES EA 1155, UFR des Sciences Pharmaceutiques et Biologiques, 1 rue Gaston Veil, 44035 Nantes, France.
authors.forename: Sophie
authors.initials: S
authors.lastname: Marhadour
authors.forename: Pascal
authors.initials: P
authors.lastname: Marchand
authors.forename: Fabrice
authors.initials: F
authors.lastname: Pagniez
authors.forename: Marc-Antoine
authors.initials: MA
authors.lastname: Bazin
authors.forename: Carine
authors.initials: C
authors.lastname: Picot
authors.forename: Olivier
authors.initials: O
authors.lastname: Lozach
authors.forename: Sandrine
authors.initials: S
authors.lastname: Ruchaud
authors.forename: Maud
authors.initials: M
authors.lastname: Antoine
authors.forename: Laurent
authors.initials: L
authors.lastname: Meijer
authors.forename: Najma
authors.initials: N
authors.lastname: Rachidi
authors.forename: Patrice
authors.initials: P
authors.lastname: Le Pape
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D047389:Casein Kinase I / Q000037:antagonists & inhibitors / Q000378:metabolism; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D018320:Leishmania major / Q000187:drug effects* / Q000201:enzymology; D008958:Models, Molecular; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D000981:Antiprotozoal Agents; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D047389:Casein Kinase I; D011493:Protein Kinase C; C001439:imidazo(1,2-a)pyridine