Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa

Autor:	Michael J. Rynkiewicz, Robert E. Babine, James E. Strickler, Harold V Meyers, Lei Jin, Frank Bibbins, Tsvetelina I. Lazarova, Joan C. Gorga
Rok vydání:	2006
Předmět:	Serine Proteinase Inhibitors Molecular model Stereochemistry Protein Conformation Clinical Biochemistry Pharmaceutical Science Crystallography X-Ray Biochemistry Chemical synthesis Factor XIa chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship Thrombin Drug Discovery medicine Structure–activity relationship Humans Molecular Biology Binding Sites biology Aryl Organic Chemistry Anticoagulants Biological activity Trypsin Boronic Acids chemistry Enzyme inhibitor Drug Design biology.protein Molecular Medicine medicine.drug Protein Binding
Zdroj:	Bioorganicmedicinal chemistry letters. 16(19)
ISSN:	0960-894X
Popis:	A series of functionalized aryl boronic acids were synthesized and evaluated as potential inhibitors of factor XIa. Crystal structures of the protein-inhibitor complexes led to the design and synthesis of second generation compounds showing single digit micromolar inhibition against FXIa and selectivity against thrombin, trypsin, and FXa.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2e5764d16a01153edfca2c4f9e71766 https://pubmed.ncbi.nlm.nih.gov/16876411 Zobrazit plný text záznamu Full Text from ScienceDirect