The pharmaceutical industry is reliant on a constant supply of new chemical entities and molecular targets for disease intervention. In this tutorial review, we want to illustrate that basic research studies on the biological function of natural products involved in plant–pathogen interactions can serve as an inspiring source for the identification of new bioactive entities as well as of strategies on how to achieve small molecule manipulation of biological systems. An application of findings from plant–pathogen interaction studies might therefore display a significant impact on drug discovery.