1000045-67-9Relevant academic research and scientific papers
Efficient synthesis of 5-amino-6-dialkylamino-4-hydroxypentanamide derivatives for renin inhibitors
Nakamura, Yuji,Ogawa, Yasuyuki,Suzuki, Chie,Fujimoto, Teppei,Miyazaki, Shojiro,Tamaki, Kazuhiko,Nishi, Takahide,Suemune, Hiroshi
, p. 1587 - 1602 (2011/08/04)
We report an efficient synthetic method for 5-amino-6-dialkylamino-4- hydroxypentanamide derivatives using Shi Asymmetric Epoxidation and the ring opening of N-(2-nitrobenzenesulfonyl)aziridine with hindered secondary amine as key steps. The Japan Institute of Heterocyclic Chemistry.
The P1 N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin
Yamaguchi, Yasuchika,Menear, Keith,Cohen, Nissim-Claude,Mah, Robert,Cumin, Frédéric,Schnell, Christian,Wood, Jeanette M.,Maibaum, Jürgen
scheme or table, p. 4863 - 4867 (2010/05/18)
Novel nonpeptide small molecule renin inhibitors bearing an N-isopropyl P1 motif were designed based on initial lead structures 1 and aliskiren (2). (P3-P1)-Benzamide derivatives such as 9a and 34, as well as the corresponding P1 basic tertiary amine derivatives 10 and 35 were found to display low nanomolar inhibition against human renin in vitro.
