2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (β-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead
A new aspartic protease inhibitory chemotype bearing a 2-amino-3,4- dihydroquinazoline ring was identified by high-throughput screening for the inhibition of BACE-1. X-ray crystallography revealed that the exocyclic amino group participated in a hydrogen
Baxter, Ellen W.,Conway, Kelly A.,Kennis, Ludo,Bischoff, Fran?ois,Mercken, Marc H.,De Winter, Hans L.,Reynolds, Charles H.,Tounge, Brett A.,Luo, Chi,Scott, Malcolm K.,Huang, Yifang,Braeken, Mirielle,Pieters, Serge M. A.,Berthelot, Didier J. C.,Masure, Stefan,Bruinzeel, Wouter D.,Jordan, Alfonzo D.,Parker, Michael H.,Boyd, Robert E.,Qu, Junya,Alexander, Richard S.,Brenneman, Douglas E.,Reitz, Allen B.
p. 4261 - 4264
(2008/03/11)
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