Discovering selective agonists of endothelial target for acetylcholine (ETA) via diversity-guided pharmacophore simplification and simulation

Two types of lead structures for selective agonists of ETA, a biological target not yet fully elucidated, has first been discovered via diversity-guided pharmacophore simplification and simulation. And it is first demonstrated that potent selective ETA agonists might be useful for protection of endothelium and for prophylaxis and treatment of cardiovascular diseases with endothelial dysfunction such as atherosclerosis and thrombosis.