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

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