Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position

Autor:	Harold G. Selnick, Lawrence C. Kuo, Kellie J. Cutrona, Bobby J. Lucas, Kristen L. Glass, Joseph P. Vacca, Youwei Yan, S. Dale Lewis, Christina L. Newton, Daniel R. McMasters, Philippe G. Nantermet, Kenneth E. Rittle, William M. Sanders, Julie A. Krueger, Matthew M. Morrissette, James C. Barrow
Rok vydání:	2003
Předmět:	biology Molecular model Molecular Structure Stereochemistry Chemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Active site Crystallography X-Ray Biochemistry Chemical synthesis Amides Antithrombins Thrombin Enzyme inhibitor Drug Discovery medicine biology.protein Molecular Medicine Potency Selectivity Molecular Biology Discovery and development of direct thrombin inhibitors medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 13(20)
ISSN:	0960-894X
Popis:	Thrombin inhibitors incorporating o -aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound in the α-thrombin–hirugen complex provides an explanation for these unanticipated results.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b3803c7c869e32f8704fe15aecff321 https://pubmed.ncbi.nlm.nih.gov/14505652 Zobrazit plný text záznamu Full Text from ScienceDirect