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Prolyl endopeptidase inhibitors
1CHINOIN Pharmaceutical and Chemical Works Ltd., Budapest, Hungary. istvan.hermecz@sanofi-synthelabo.com
Abstract:
Selective prolyl endopeptidase inhibitors were elaborated by modification of the structure of SUAM-1221, by using a CoMFA study and protein crystallography. The most active representatives of omega-(N-hetaryl)alkanoylprolylpyrrolidines, containing 2- or 3-methylene chain links have high activity (IC50 10(-9)-10(-11)) and exhibit significant in vivo activities.