Document Detail

Discovery of novel non-peptidic ketopiperazine-based renin inhibitors.
MedLine Citation:
PMID:  15755665     Owner:  NLM     Status:  MEDLINE    
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).
Daniel D Holsworth; Noel A Powell; Dennis M Downing; Cuiman Cai; Wayne L Cody; J Michael Ryan; Robert Ostroski; Mehran Jalaie; John W Bryant; Jeremy J Edmunds
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  13     ISSN:  0968-0896     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2005 Apr 
Date Detail:
Created Date:  2005-03-09     Completed Date:  2005-09-01     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  2657-64     Citation Subset:  IM    
Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. <>
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MeSH Terms
Blood Pressure / drug effects
Enzyme Inhibitors / chemical synthesis,  chemistry,  pharmacology*
Mice, Transgenic
Molecular Structure
Piperazines / chemical synthesis,  chemistry,  pharmacology*
Renin / antagonists & inhibitors*
Structure-Activity Relationship
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Piperazines; EC

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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