777934-44-8Relevant academic research and scientific papers
Discovery of novel non-peptidic ketopiperazine-based renin inhibitors
Holsworth, Daniel D.,Powell, Noel A.,Downing, Dennis M.,Cai, Cuiman,Cody, Wayne L.,Ryan, J. Michael,Ostroski, Robert,Jalaie, Mehran,Bryant, John W.,Edmunds, Jeremy J.
, p. 2657 - 2664 (2005)
Ketopiperazine 2 was designed from a previously published analog. Compound 2 was shown to be a novel, potent inhibitor of renin that, when administered orally, lowered blood pressure in a hypertensive double transgenic (human renin and angiotensinogen) mouse model. Compound 2 was further optimized to sub-nanomolar potency by designing an analog that addressed the S3 sub-pocket of the renin enzyme (16).
PIPERAZINE DERIVATIVE RENIN INHIBITORS
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Page 61-62, (2010/02/09)
Disclosed are piperazine derivatives, their manufacture and use as inhibitors of renin. Formula (I):
