Premium
The spinosyns, spinosad, spinetoram, and synthetic spinosyn mimics ‐ discovery, exploration, and evolution of a natural product chemistry and the impact of computational tools
Author(s) -
Sparks Thomas C,
Crouse Gary D,
Benko Zoltan,
Demeter David,
Giampietro Natalie C,
Lambert William,
Brown Annette V
Publication year - 2021
Publication title -
pest management science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.296
H-Index - 125
eISSN - 1526-4998
pISSN - 1526-498X
DOI - 10.1002/ps.6073
Subject(s) - spinosad , natural product , biochemical engineering , microbiology and biotechnology , chemistry , biology , pesticide , ecology , engineering , biochemistry
Abstract Natural products (NPs) have long been a source of insecticidal crop protection products. Like many macrolide NPs, the spinosyns originated from a soil inhibiting microorganism ( Saccharopolyspora spinosa ). More than 20 years after initial registration, the spinosyns remain a unique class of NP‐based insect control products that presently encompass two insecticidal active ingredients, spinosad, a naturally occurring mixture of spinosyns, and spinetoram, a semi‐synthetic spinosyn product. The exploration and exploitation of the spinosyns has, unusually, been tied to an array of computational tools including artificial intelligence (AI)‐based quantitative structure activity relationship (QSAR) and most recently computer‐aided modeling and design (CAMD). The AI‐based QSAR directly lead to the discovery of spinetoram, while the CAMD studies have recently resulted in the discovery and building of a series of synthetic spinosyn mimics. The most recent of these synthetic spinosyn mimics show promise as insecticides targeting lepidopteran insect pests as demonstrated by field studies wherein the efficacy has been shown to be comparable to spinosad and spinetoram. These and a range of other aspects related to the exploration of the spinosyns over the past 30 years are reviewed herein. © 2020 Society of Chemical Industry