ABSTRACT
This chapter describes the detail of recent synthetic work on the marine macrolide zampanolide and discusses how this work has allowed to address questions of biological relevance and/or has led to structurally simplified templates for further medicinal chemistry research. The vast majority of natural product–derived drugs as of today originate from terrestrial organisms. Marine secondary metabolites have served as starting points for successful drug development, although the number of marine natural product–derived marketed drugs at this point in time is still limited. From a medicinal chemistry perspective, the chemistry developed in the course of a total synthesis provides the basis for structure–activity relationship (SAR) studies in areas of structural space that are not accessible either through semisynthesis or the genetic manipulation of producer organisms. Natural products of marine origin hold a distinct position, in light of their enormous structural diversity and broad range of biological activities.
