Abstract: Natural products are an important resource for pharmaceutical development. From the mixed biogenesis of polyketide-terpenoid origin, drimane quinones/hydroquinones have attracted widespread attention by chemists and biologists for their unique structures and diverse biological activities. This class of natural products were made up of drimane or rearranged drimane connected with quinone or hydroquinone via C(sp²)-C(sp³) linker. Zonarol was isolated as a typical drimane meroterpenoid with antifungal activity. It was later demonstrated to have anti-feeding activity, antitumor activity, anti-inflammatory activity, algicidal activity, which have good potential for the discovery of novel pharmaceutical leads. The advances in the synthesis, structure optimization and biological activity of zonarol and its analogues were showcased, aiming for the practical optimization and pharmacological studies. This may serve as a useful inspiration for the discovery of new agrochemicals.