Discovery of imidazo[1,2-a]pyridine-based anthelmintic targeting cholinergic receptors of Haemonchus Contortus

Publication date: Available online 6 November 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Jean-Paul Déto Ursul N'Guessan, Pierre-Olivier Delaye, Mélanie Pénichon, Claude L. Charvet, Cédric Neveu, Mahama Ouattara, Cécile Enguehard-Gueiffier, Alain Gueiffier, Hassan Allouchi
We report the synthesis of a series of imidazo[1,2-a]pyridine-based molecules as anthelmintic against the livestock parasite Haemonchus contortus. The molecules were tested by using Larval Paralysis Test (LPT), in order to target ionic channels, as most of the prominent marketed anthelminthics present such mechanism of action. The most active compound (5e) displayed paralysis on H. contortus stage 3 larvae until 31.25µM. Effect of 5e on H. contortus cholinergic receptors (L-AChR1 and 2) was characterized via electrophysiological measurement and a rare antagonist mode of action was unveiled.

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