943924-39-8Relevant articles and documents
Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application
Lerchner, Andreas,Machauer, Rainer,Betschart, Claudia,Veenstra, Siem,Rueeger, Heinrich,McCarthy, Clive,Tintelnot-Blomley, Marina,Jaton, Anne-Lise,Rabe, Sabine,Desrayaud, Sandrine,Enz, Albert,Staufenbiel, Matthias,Paganetti, Paolo,Rondeau, Jean-Michel,Neumann, Ulf
scheme or table, p. 603 - 607 (2010/06/19)
A series of macrocyclic peptidic BACE-1 inhibitors was designed. While potency on BACE-1 was rather high, the first set of compounds showed poor brain permeation and high efflux in the MDRI-MDCK assay. The replacement of the secondary benzylamino group wi