Design, Synthesis, and Structure—Activity Relationship of a New Class of Amidinophenylurea-Based Factor VIIa Inhibitors

Autor:	Hans Matter, Manfred Schudok, Martin Lorenz, Peter Wildgoose, Hans Peter Nestler, Otmar Klingler, S. Paul Bajaj, Joerg Czech, Herman Schreuder
Rok vydání:	2003
Předmět:	Models Molecular Molecular model Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide Factor VIIa Selective inhibition Crystallography X-Ray Biochemistry Chemical synthesis Amidine chemistry.chemical_compound Structure-Activity Relationship Antithrombotic treatment Drug Discovery medicine otorhinolaryngologic diseases Humans Structure–activity relationship Molecular Biology biology Chemistry Phenylurea Compounds Organic Chemistry Coagulation factor VIIa General Medicine Combinatorial chemistry Design synthesis Enzyme inhibitor Drug Design biology.protein Molecular Medicine sense organs
Zdroj:	ChemInform. 34
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200331252
Popis:	Selective inhibition of coagulation factor VIIa has recently gained attraction as interesting approach towards antithrombotic treatment. Using parallel synthesis supported by structure-based design and X-ray crystallography, we were able to identify a novel series of amidinophenylurea derivatives with remarkable affinity for factor VIIa. The most potent compound displays a Ki value of 23 nM for factor VIIa.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81bb22de0780fdf943fd66180c741dbd https://doi.org/10.1002/chin.200331252 Zobrazit plný text záznamu Plný text