A stereoselective approach to peptidomimetic BACE1 inhibitors

…, M Brindisi, S Giovani, S Maramai, G Kshirsagar…

Index: Butini, Stefania; Gabellieri, Emanuele; Brindisi, Margherita; Giovani, Simone; Maramai, Samuele; Kshirsagar, Giridhar; Guarino, Egeria; Brogi, Simone; La Pietra, Valeria; Giustiniano, Mariateresa; Marinelli, Luciana; Novellino, Ettore; Campiani, Giuseppe; Cappelli, Andrea; Gemma, Sandra European Journal of Medicinal Chemistry, 2013 , vol. 70, p. 233 - 247

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Citation Number: 11

Abstract

Abstract Aiming at identifying new scaffolds to generate beta-secretase (BACE1) inhibitors we developed peptidomimetics based on a 1, 4-benzodiazepine core (3a–d), their seco- analogs (4a–b), and linear analogs (5a–h), by stereoselective approaches. We herein discuss the synthesis, molecular modeling and in vitro studies for the newly developed ligands. Compounds 5c and 5h behaved as BACE1 inhibitors on the isolated enzyme and ...