Retro-Binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity

Autor:	Daniel G.M. Roberts, Wan F. Lau, Wen-Ching Han, Martin L. Ogletree, William A. Schumacher, Tammy C. Wang, James Lin, Edwin J. Iwanowicz, S. David Kimball, Steven M. Seiler
Rok vydání:	2002
Předmět:	Serine Proteinase Inhibitors Clinical Biochemistry Pharmaceutical Science Peptide Biochemistry Catalysis Mice Structure-Activity Relationship Thrombin In vivo Drug Discovery medicine Animals Humans Molecular Biology chemistry.chemical_classification Binding Sites biology Organic Chemistry Active site Biological activity In vitro Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine Oligopeptides circulatory and respiratory physiology medicine.drug
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 12:3183-3186
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(02)00651-0
Popis:	A series of retro-binding inhibitors of human α-thrombin was prepared to elucidate structure–activity relationships (SAR) and optimize in vivo performance. Compounds 9 and 11, orally active inhibitors of thrombin catalytic activity, were identified to be efficacious in a thrombin-induced lethality model in mice.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8346fdc4173a6da63c59cb90b9947c4 https://doi.org/10.1016/s0960-894x(02)00651-0 Zobrazit plný text záznamu Full Text from ScienceDirect