New Perspectives in Exploiting Secondary Metabolite Glycosides as Drug Leads

Abstract

Plant secondary metabolites (SM), which frequently occur as glycosides, constitute large pool of structures which are valuable for medicinal chemistry and molecular pharmacology because of their inherent biocompatibility. Despite rich ethnopharmacological tradition of their application, glycosides as individual chemical entities are not very frequent as therapeutic agents, and their bulk availability is usually low. The current potential of chemical synthetic methods of glycosylation is discussed, in context of structural diversity needs in contemporary drug discovery programs. Newly designed procedures for glycosylation, which rely on transition metal catalysis, together with already established methods of chemical ligation (click chemistry), are well suited for elaboration of new semisynthetic SM libraries based on chemical glycosylation and glycorandomization principles