SIVANTO™ - discovery of a new butenolide insecticide

The nicotinic acetylcholine receptor is one of the most important molecular target sites for insecticidal activity and plays a central role in the mediation of fast excitatory synaptic transmission in the insect central nervous system. The discovery of SIVANTO™, an innovative insecticide from the new class of butenolides, was inspired by the natural product stemofoline (isolated from the plant Stemona japonica) and relevant neonicotinoid ligands. Compared with already commercialized neonicotinoids, SIVANTO™ contains a different pharmacophore system as new bioactive scaffold, which is responsible for its specific physicochemical properties, systemicity, metabolism in plants and insects, and for a favorable safety profile. Due to its fast uptake, translamination and distribution in plants, SIVANTO™ has a high degree of versatility in application methods in a variety of crops, exhibiting excellent and fast efficacy against a broad-spectrum of sucking pests. First details around the discovery of SIVANTO™ and the structure-activity relationship of a series of butenolides will be presented.