Pyruvate dehydrogenase (PDH), multienzyme complexes responsible for the conversion of pyruvate to acetyl coenzyme A, is well known as a site of action of pesticides. Phosphinates and phosphonates are structural analogues of pyruvic acid in which the carboxylic group is replaced by a phosphonic or related moiety. Many phosphinates and phosphonates have been confirmed as very powerful inhibitors of PDH and also being herbicidal, but none of them were active enough to be commercialized.We began a systemati...