Novel, potent non-covalent thrombin inhibitors incorporating p(3)-lactam scaffolds
| Autor: | Tony Gibson, J. Edward Semple, Jonathan Zhangi Ho |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Lactams
medicine.drug_class Stereochemistry Peptidomimetic Clinical Biochemistry Pharmaceutical Science Biological Availability Carboxamide Biochemistry Chemical synthesis Antithrombins Amidine chemistry.chemical_compound Structure-Activity Relationship Thrombin Dogs Drug Discovery medicine Animals Trypsin Molecular Biology Blood Coagulation biology Molecular Structure Organic Chemistry Serine Endopeptidases Combinatorial chemistry chemistry Enzyme inhibitor Lactam biology.protein Molecular Medicine Discovery and development of direct thrombin inhibitors medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 12(5) |
| ISSN: | 0960-894X |
| Popis: | Evolution of P 1 -argininal inhibitor prototypes led to a series of non-covalent P 3 -7-membered lactam inhibitors 1a – w , featuring novel peptidomimetic units that probe each of the S 1 , S 2 , and S 3 specificity pockets of thrombin. Rigid P 1 -arginine surrogates possessing a wide range of basicity (calcd p K a 's∼neutral–14) were surveyed. The design, synthesis, and biological activity of these targets are presented. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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