Chemical postevolution

Chemical Postevolution is the optimization of (already evolutionary optimized) natural products by synthetic chemical means. It is additional and often structurally orthogonal to natural evolution. Natural products have provided the majority of lead structures for marketed antibiotics. But, only a few “pure” natural products fulfill the complex profile required for a pharmaceutical drug. A drug has to match additional physicochemical, pharmacological, toxicological and technical requirements that have not been selectors in the evolution of antibacterial secondary metabolites. On the other hand, natural products offer excellent starting points for medicinal chemistry. To create a drug, nature’s blueprints often have to be improved by semisynthesis or de novo synthesis to repair typical deficiencies such as limited stability, low solubility, narrow antibacterial spectrum, poor in vivo efficacy, etc. Chemical structure defines biological activity. Complementary to nature, a chemist can explore white spots in structural space and biological activity that have never been touched by any organism over the entire period of evolution.