2. Academic Validation
  3. Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo

Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo

  • Bioorg Med Chem Lett. 2009 Mar 1;19(5):1366-70. doi: 10.1016/j.bmcl.2009.01.055.
Rainer Machauer 1,  Kurt Laumen,  Siem Veenstra,  Jean-Michel Rondeau,  Marina Tintelnot-Blomley,  Claudia Betschart,  Anne-Lise Jaton,  Sandrine Desrayaud,  Matthias Staufenbiel,  Sabine Rabe,  Paolo Paganetti,  Ulf Neumann
Affiliations

Affiliation

  • 1 Novartis Institutes for BioMedical Research, Novartis Pharma AG, PO Box, CH-4002 Basel, Switzerland.
PMID: 19195887 DOI: 10.1016/j.bmcl.2009.01.055
Abstract

The macrocyclic peptidic BACE-1 inhibitors 2a-c show moderate enzymatic and cellular activity. By exchange of the hydroxyethylene- to ethanolamine-transition state mimetic the peptidic character was reduced, providing the highly potent and selective inhibitor 3. Variation of the P' moiety resulted in the macrocyclic inhibitor 14. Both macrocycles show inhibition of BACE-1 in the brain of APP51/16 transgenic mice, 3 (NB-544) after intravenous and 14 (NB-533) after oral application.

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