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Your search keyword '"Oxacephem"' showing total 2 results
Start Over Descriptor "Oxacephem" Journal bioorganicmedicinal chemistry letters
2 results on '"Oxacephem"'

1. Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors

Author

Noriyuki Naya, Yasuhiro Nishitani, Masatoshi Nakajima, Akiko Kanda, Masaaki Uenaka, Toshiro Konoike, Yasuyoshi Iso, and Yasunori Aoyama

Subjects
Serine Proteinase Inhibitors, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Chemical synthesis, Serine, chemistry.chemical_compound, Structure-Activity Relationship, Chymases, Drug Discovery, Humans, Molecular Biology, Oxacephem, chemistry.chemical_classification, biology, Molecular Structure, Organic Chemistry, Serine Endopeptidases, Chymase, In vitro, Cephalosporins, Enzyme, chemistry, Enzyme inhibitor, Drug Design, biology.protein, Lactam, Molecular Medicine
Abstract

1-Oxacephem derivatives were synthesized and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 1-oxacephems led to compound 34, which exhibited 6 nM inhibition of human chymase and high selectivity for human chymase compared to other serine enzymes.

Published
2000

2. 1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma

Author

Yasuhiro Nishitani, Yasunori Aoyama, Toshiro Konoike, Masatoshi Nakajima, Yasuyoshi Iso, Akiko Kanda, Masaaki Uenaka, and Noriyuki Naya

Subjects
Models, Molecular, Serine Proteinase Inhibitors, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, Chemical synthesis, chemistry.chemical_compound, Plasma, Structure-Activity Relationship, Chymases, Drug Discovery, Enzyme Stability, Structure–activity relationship, Humans, Molecular Biology, Oxacephem, chemistry.chemical_classification, biology, Molecular Structure, Organic Chemistry, Serine Endopeptidases, Chymase, In vitro, Cephalosporins, Enzyme, chemistry, Enzyme inhibitor, biology.protein, Lactam, Molecular Medicine
Abstract

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).

Published
2000

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