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New potent prolyl endopeptidase inhibitors: Synthesis and structure-activity relationships of indan and tetralin derivatives and their analogs

…, T Yamanaka, M Torizuka, K Yoshinaga…

文献索引:Tanaka; Niwa; Nishioka; Yamanaka; Torizuka; Yoshinaga; Kobayashi; Ikeda; Arai Journal of Medicinal Chemistry, 1994 , vol. 37, # 13 p. 2071 - 2078

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被引用次数: 41

摘要

Prolyl endopeptidase (PEP)[EC 3.4. 21.261 is a serine protease that specifically cleaves peptidyl proline bonds.'This enzyme hydrolyzes many biologically active peptides, including thyrotropin-releasing hormone, substance P, angiotensin 11, oxytocin, and bradykinin.-The enzyme also degrades arginine vasopressin which may facilitate learning and mem~ ry.~-~ Yoshimoto et al. reported that the PEP inhibitor 1-[1-(benzyloxycarbonyl)-~-prolyl] prolinal ...