Prolyl endopeptidase inhibitors

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 ω-( N-hetaryl)alkanoylprolylpyrrolidines, containing 2- or 3-methylene chain links have high activity (IC 50...

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Veröffentlicht in:	Farmaco (Società chimica italiana : 1989) 2000-03, Vol.55 (3), p.188-190
Hauptverfasser:	Hermecz, István, Kánai, Károly
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals CoMFA Crystallography Endopeptidases - metabolism In Vitro Techniques Prolyl endopeptidase inhibitors Protease Inhibitors - chemical synthesis Protease Inhibitors - pharmacology Protein crystallography Pyrroles - chemical synthesis Pyrroles - pharmacology Rats Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - pharmacology Structure-Activity Relationship Synthesis ω-( N-Hetaryl)alkanoylprolylpyrrolidines
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Beschreibung
Zusammenfassung:	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 ω-( N-hetaryl)alkanoylprolylpyrrolidines, containing 2- or 3-methylene chain links have high activity (IC 50 10 −9∼10 −11) and exhibit significant in vivo activities.
ISSN:	0014-827X 1879-0569
DOI:	10.1016/S0014-827X(00)00018-5