Discovery of Imidazopyridine Derivatives as Highly Potent Respiratory Syncytial Virus Fusion Inhibitors

摘要

A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and physical-chemical properties. Several highly potent compounds such as 8ji, 8j1, and 8jm were identified with single nanomolar activities. The most potent compound 8jrn showed an IC50 of 3 nM, lower nnicrosome clearance and no CYP inhibition. The profile of 8jrn appeared to be superior to BMS433771, and supported further optimization.