| Renin inhibitors containing alpha-heteroatom amino acids as P2 residues. | |
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MedLine Citation:
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PMID: 1552498 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A series of renin inhibitors having alpha-heteroatom amino acids as P2 substitutions has been prepared. Examples where the heteroatom is oxygen, sulfur, or nitrogen are described. Many of the compounds exhibit subnanomolar potency when tested in vitro against monkey renin. When selected compounds were tested orally in conscious, salt-depleted, normotensive, Cynomolgus monkeys, low to moderate blood pressure lowering was observed. At an oral dose of 30 mg/kg, compound 53a lowered blood pressure by a maximum of 18 mmHg at 2.5 h post-dose. |
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Authors:
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J T Repine; J S Kaltenbronn; A M Doherty; J M Hamby; R J Himmelsbach; B E Kornberg; M D Taylor; E A Lunney; C Humblet; S T Rapundalo |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 35 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 1992 Mar |
Date Detail:
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Created Date: 1992-04-28 Completed Date: 1992-04-28 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1032-42 Citation Subset: IM |
Affiliation:
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Department of Chemistry, Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48106-1047. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Amino Acids
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chemical synthesis*,
pharmacology Animals Blood Pressure / drug effects Cathepsin D / antagonists & inhibitors Cattle Glyoxylates / chemical synthesis*, pharmacology Macaca fascicularis Male Models, Molecular Renin / antagonists & inhibitors* Stereoisomerism Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Amino Acids; 0/Glyoxylates; EC 3.4.23.15/Renin; EC 3.4.23.5/Cathepsin D |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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