Sulfonimidamides in Medicinal and Agricultural Chemistry

Angew Chem Int Ed Engl. 2017 Apr 3;56(15):4100-4109. doi: 10.1002/anie.201610456. Epub 2017 Feb 23.


The synthesis and evaluation of structural analogues and isosteres are of central importance in medicinal and agricultural chemistry. The sulfonamide functional group represents one of the most important amide isosteres in contemporary drug design, and about 500 such compounds have overcome both the pharmacological and regulatory hurdles that precede studies in humans. The mono aza analogues of sulfonamides, that is, sulfonimidamides, are rapidly gaining popularity as a novel functional group among synthetic chemists involved in the design of biologically active compounds for both pharmaceutical and agrochemical applications. Herein, we review these recent developments to showcase the promise of this functional group.

Keywords: agricultural chemistry; bioisosteres; drug design; medicinal chemistry; sulfonimidamides.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Chemistry, Agricultural*
  • Chemistry, Pharmaceutical*
  • Drug Design
  • Humans
  • Molecular Structure
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology*


  • Sulfonamides