Recent advances in avermectin chemistry

One half of the 2015 Nobel Prize in Physiology or Medicine was awarded to Satoshi Omura and William Campbell for the discovery of natural avermectins in 1976, which has revolutionized the treatment of endo- and ectoparasitic diseases. The published reviews on avermectins are primarily concerned with their biological activity and applications. This is the first review that analyzes the main advances and trends in the development of avermectin chemistry. The strategies for the total synthesis of natural avermectins are described. Considerable attention is given to the methods of chemical modification of avermectins giving new semisynthetic derivatives. The established structure–biological activity relationships for the products are discussed. The review considers the optimal strategies for chemical modification of avermectins in order to increase their biological activity and stability, reduce toxicity for warm-blooded animals and expand their field of application.
Bibliography — 241 references.