P3 cap modified Phe*-Ala series BACE inhibitors

Autor: Jason Eric Lamar, Jon A. Erickson, Todd J. Kohn, Mccarthy James R, Hsiu-Chiung Yang, Guo Deqi, Patrick C. May, Shu-Hui Chen, David E. Timm, Yip Yvonne Yee Mai, James McGee
Rok vydání: 2003
Předmět:
Zdroj: Bioorganicmedicinal chemistry letters. 14(1)
ISSN: 0960-894X
Popis: With the aim of reducing molecular weight and adjusting log D value of BACE inhibitors to more favorable range for BBB penetration and better bioavailability, we synthesized and evaluated several series of P3 cap modified BACE inhibitors obtained via replacement of the P3NHBoc moiety as seen in 3 with other polar functional groups such as amino, hydroxyl and fluorine. Several promising inhibitors emerging from this P3 cap SAR study (e.g., 15 and 19) demonstrated good enzyme inhibitory potencies (BACE-1 IC(50)
Databáze: OpenAIRE
načítá se...