1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma

1-Oxacephem derivatives were evaluated as a novel series of chymase inhibitors. The structure–activity relationship studies of 1-oxacephems led to compounds 15, which exhibited 27 nM inhibition of human chymase and improvement of stability in human plasma ( t 1/2 1.5 h).

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-11, Vol.10 (21), p.2403-2406
Main Authors: Aoyama, Yasunori, Uenaka, Masaaki, Konoike, Toshiro, Iso, Yasuyoshi, Nishitani, Yasuhiro, Kanda, Akiko, Naya, Noriyuki, Nakajima, Masatoshi
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cardiovascular system
Cephalosporins - blood
Cephalosporins - chemical synthesis
Cephalosporins - chemistry
Cephalosporins - pharmacology
Chymases
Enzyme Stability
Humans
Medical sciences
Miscellaneous
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Plasma - chemistry
Serine Endopeptidases - chemistry
Serine Endopeptidases - metabolism
Serine Proteinase Inhibitors - blood
Serine Proteinase Inhibitors - chemical synthesis
Serine Proteinase Inhibitors - chemistry
Serine Proteinase Inhibitors - pharmacology
Structure-Activity Relationship
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Description
Summary:1-Oxacephem derivatives were evaluated as a novel series of chymase inhibitors. The structure–activity relationship studies of 1-oxacephems led to compounds 15, which exhibited 27 nM inhibition of human chymase and improvement of stability in human plasma ( t 1/2 1.5 h).
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00489-3