【文章名】The P-1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin
The P-1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin
[摘要]：Novel nonpeptide small molecule renin inhibitors bearing an N-isopropyl P-1 motif were designed based on initial lead structures 1 and aliskiren (2). (P-3-P-1)-Benzamide derivatives such as 9a and 34, as well as the corresponding P-1 basic tertiary amine derivatives 10 and 35 were found to display low nanomolar inhibition against human renin in vitro. (C) 2009 Elsevier Ltd. All rights reserved.
