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Insertion of Small Flexible Linkers as a Useful Scaffold Hopping Tool in Agrochemistry

Journal

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
Volume 70, Issue 36, Pages 11011-11018

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jafc.1c07971

Keywords

insertion; elongation; herbicide; fungicide; insecticide; agrochemical; crop protection

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This article highlights the significance of manipulating molecular backbones by inserting small flexible linkers and demonstrates how analogues derived through this strategy may exhibit similar biological activity. Elongation with oxygen, amino, methylene, ethylene, vinyl, ethynyl, and CH2O bridges has led to the discovery of highly active agrochemicals.
Inserting small flexible linkers of only one-to three-atom chain lengths into a molecular backbone is an important scaffold hopping manipulation. Analogues derived from biologically active compounds through the utilization of such a strategy are often similar in shape and physicochemical properties and, therefore, likely to exhibit similar potency. This review will demonstrate how the elongation with oxygen, amino, methylene, ethylene, vinyl, ethynyl, and CH2O bridges led to the discovery of highly active agrochemicals.

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