Effect of cyclo-alkyl lactamimides upon human pepsins and pepsinogens.
1. Eight cyclo-alkyl lactamimides have been investigated for potential inhibitory action upon the pepsins and pepsinogens. 2. Human pepsins 1, 3 and 5 and swine pepsin were inhibited only slightly. 2. Human and swine pepsinogens were inactivated progressively by lactamimides as the number of methylene groups in the nitrogen-containing ring increased. The most potent inactivator studied was N-(cis-2-phenylcyclopentyl)-azacyclotridecan-2-imine hydrochloride. 4. Substitution of benzyl and tertiary butyl groups in the N-containing ring increased the pepsinogen-inactivating property of the cyclo-alkyl lactamimides. 5. N-(cis-2-Phenylcyclopentyl)azacyclotridecan-2-imine hydrochloride may be of potential importance as a therapeutic agent in peptic ulcer, and modifications to the molecule which might increase its pepsinogen-inactivating ability are suggested.
D006801:Humans; D007094:Imides / Q000494:pharmacology* / Q000627:therapeutic use; D010434:Pepsin A / Q000037:antagonists & inhibitors*; D010435:Pepsinogens / Q000037:antagonists & inhibitors*; D010437:Peptic Ulcer / Q000188:drug therapy; D013329:Structure-Activity Relationship
D007094:Imides; D010435:Pepsinogens; D010434:Pepsin A