Increased activity of CF₃-derivatized levamisole at the ACC-2 receptor from the parasitic nematode Haemonchus contortus.

ABSTRACT: The acetylcholine-gated chloride channel (ACC) family in parasitic nematodes represents a promising target for anthelmintic drug development. Levamisole, a widely known and utilized cholinergic agonist, has been used for decades to address many types of parasitic infections by targeting nematode nicotinic acetylcholine receptors (nAChRs) in nematodes. In this study, we report the synthesis and pharmacological evaluation of eight levamisole derivatives, five of which are novel, on the H. contortus ACC-2 receptor. This includes a CF₃-derivatized compound we have identified as compound 6 whose structure contains levamisole as a backbone with the addition of a 2-trifluoromethyl benzyl group. Electrophysiological assays revealed that compound 6 exhibited a five-fold increase in sensi

SUBMITTER: Collins A 

PROVIDER: S-EPMC11930178 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature