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 31.25 µM. 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.

中文翻译：

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发现基于咪唑并[1,2- a ]吡啶的驱虫靶向性对捻转血矛线虫胆碱能受体

我们报告了一系列基于咪唑并[1,2 - a ]吡啶的分子的合成，作为驱虫剂对抗牲畜寄生虫Haemonchus contortus。为了靶向离子通道，通过使用幼虫麻痹测试（LPT）对分子进行了测试，因为大多数市售的驱虫药都具有这种作用机理。最活跃的化合物（图5e）显示麻痹上捻转血矛线虫阶段3幼虫直到31.25μM。的效果5E对捻转血矛线虫胆碱能受体（L-AChR1和2）的特征在于通过电生理测量和动作的一个罕见的拮抗剂模式被推出。