Phenoxyalkyl cyclic and acyclic amine derivatives: what do they teach us about scaffold-based drug design?

Abstract

Fragment-based drug design of new bioactive scaffolds is a recent aspect of medicinal chemistry that provides a faster and more efficient road in drug discovery. Phenoxyethyl piperidine and morpholine derivatives have various pharmacological activities, from antitussive to anticancer properties. They are also widely used in selective estrogen receptor modulator (SERM) drugs and can be used to prevent osteoporosis in postmenopausal women. Also, other recent findings suggest that these compounds exhibit high anticholinergic and H₃ inverse agonistic activities. We outlined the process of developing novel medications for Alzheimer’s disease, malaria, cancer, and various other illnesses, which could entail modifying or incorporating these structures into a different biologically active framework. Pharmacokinetic assessment and organic pathways for synthesizing these scaffolds are also indicated. This review will discuss the recent pharmaceutical advances of phenoxyethyl cyclic amine derivatives in experimental, investigational, and FDA-approved drugs to draw an apparent viewpoint for future drug research and discovery.