title: Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives.
abstract: The synthesis of two new series of dicarboxylic acid dipeptides and two sulfhydryl-containing inhibitors are described. The in vitro enkephalinase inhibition data and some in vivo analgesic data are presented for these compounds. For the dibenzylglutaric acid series structure-activity relationships and in vivo analgesic activity are discussed. The reverse amides, i.e., 4-amino-2,4-dibenzylbutyric acid derivatives, are also discussed. Two sulfhydryl-containing inhibitors showed good in vivo potency in the mouse jump-latency hot-plate test after peripheral administration at moderate low doses.
authors.affiliation: Research Department, CIBA-GEIGY Corporation, Summit, New Jersey 07901.
authors.forename: G M
authors.initials: GM
authors.lastname: Ksander
authors.forename: C G
authors.initials: CG
authors.lastname: Diefenbacher
authors.forename: A M
authors.initials: AM
authors.lastname: Yuan
authors.forename: F
authors.initials: F
authors.lastname: Clark
authors.forename: Y
authors.initials: Y
authors.lastname: Sakane
authors.forename: R D
authors.initials: RD
authors.lastname: Ghai
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis; D000818:Animals; D001593:Benzyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D001812:Blood-Brain Barrier; D055598:Chemical Phenomena; D002621:Chemistry; D003461:Crystallography; D005977:Glutarates / Q000138:chemical synthesis / Q000494:pharmacology*; D008297:Male; D051379:Mice; D015260:Neprilysin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D001593:Benzyl Compounds; D005977:Glutarates; D015260:Neprilysin