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.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antineoplastic Agents / chemical synthesis
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology*
-
Antiprotozoal Agents / chemical synthesis
-
Antiprotozoal Agents / chemistry
-
Antiprotozoal Agents / pharmacology*
-
Casein Kinase I / antagonists & inhibitors
-
Casein Kinase I / metabolism
-
Cell Proliferation / drug effects
-
Dose-Response Relationship, Drug
-
Drug Screening Assays, Antitumor
-
HeLa Cells
-
Humans
-
Leishmania major / drug effects*
-
Leishmania major / enzymology
-
Models, Molecular
-
Molecular Structure
-
Parasitic Sensitivity Tests
-
Protein Kinase C / antagonists & inhibitors
-
Protein Kinase C / metabolism
-
Protein Kinase Inhibitors / chemical synthesis
-
Protein Kinase Inhibitors / chemistry
-
Protein Kinase Inhibitors / pharmacology*
-
Pyridines / chemical synthesis
-
Pyridines / chemistry
-
Pyridines / pharmacology*
-
Structure-Activity Relationship
Substances
-
Antineoplastic Agents
-
Antiprotozoal Agents
-
Protein Kinase Inhibitors
-
Pyridines
-
Casein Kinase I
-
Protein Kinase C
-
imidazo(1,2-a)pyridine