| abstract |
PURPOSE: To provide a novel compound having a prolyl endopeptibase activity- inhibiting action and useful as an anti-dement agent, especially an anti-amnestic agent. n CONSTITUTION: A compound of formula I [X is COR 1 , CO 2 R 2 , SO 2 R 3 , etc., (R 1 -R 3 are H, 1-15C hydrocarbon, etc.,); Y, Z are methine, N; A is single bond, methylene, 2-3C polymethylene; B is methylene, 2-3C polymethylene; W is amino acid residue,-D-CO-(D is 1-4C alkylene, etc.,); n is 0,1; C is -OR 9 , -N(R 10 )(R 11 ) (R 9 is 1-10C hydrocarbon; R 10 , R 11 can be combined with each other into a substitutable cyclic ring group)], e.g. N-(D,L-1-benzyloxycarbonylpiperidine-2- carbonyl)(L)-methionine ethyl ester. The compound of formula I is produced by reacting a compound of formula II with a compound of formula: E 2 -(W) n -C(E 2 is the same as E 1 ) in the presence of a condensing agent (e.g. carbonyldiimidazole) in a solvent such as THF at -20 to 30°C. n COPYRIGHT: (C)1992,JPO&Japio |