Design, Synthesis, and Structure—Activity Relationship of a New Class of Amidinophenylurea-Based Factor VIIa Inhibitors
العنوان: | Design, Synthesis, and Structure—Activity Relationship of a New Class of Amidinophenylurea-Based Factor VIIa Inhibitors |
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المؤلفون: | Hans Matter, Manfred Schudok, Martin Lorenz, Peter Wildgoose, Hans Peter Nestler, Otmar Klingler, S. Paul Bajaj, Joerg Czech, Herman Schreuder |
المصدر: | ChemInform. 34 |
بيانات النشر: | Wiley, 2003. |
سنة النشر: | 2003 |
مصطلحات موضوعية: | 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 |
الوصف: | 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. |
تدمد: | 1522-2667 0931-7597 |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81bb22de0780fdf943fd66180c741dbd https://doi.org/10.1002/chin.200331252 |
حقوق: | CLOSED |
رقم الأكسشن: | edsair.doi.dedup.....81bb22de0780fdf943fd66180c741dbd |
قاعدة البيانات: | OpenAIRE |
تدمد: | 15222667 09317597 |
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