Discovery of human GPCR antagonists with potent in vitro and in vivo Macrofilaricidal activity: A potential new treatment for River Blindness
Filarial worms cause serious, sometimes life-threatening disease, including River Blindness in humans and heartworm in dogs plus other costly ailments in livestock. Here we perform hit to lead identification studies on the 4 FDA-approved human GPCR antagonists, clemizole, pimozide, proroxan, and suloctidil as novel antifilarial drugs. One of the lead compounds, clemizole analog C-8 was tested in vivo against adult Brugia pahangi to identify differentially expressed genes of interest.