1-(2-Naphthyl)-1 H -pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs

Autor:	Yanhong Wu, Ann E. Arfsten, Bing-Yan Zhu, Uma Sinha, Lane A. Clizbe, Penglie Zhang, Robert M. Scarborough, Susan Edwards, Erick A. Goldman, Merlyn Alphonso, Athiwat Hutchaleelaha, Wenrong Huang, Zhaozhong J. Jia
Rok vydání:	2004
Předmět:	medicine.drug_mechanism_of_action medicine.drug_class Stereochemistry Antithrombin III Clinical Biochemistry Factor Xa Inhibitor Pharmaceutical Science Carboxamide Pyrazole Biochemistry Chemical synthesis Rats Sprague-Dawley chemistry.chemical_compound Drug Discovery medicine Animals Humans Potency Molecular Biology chemistry.chemical_classification biology Organic Chemistry Amides In vitro Rats Enzyme chemistry Enzyme inhibitor biology.protein Pyrazoles Molecular Medicine Factor Xa Inhibitors Protein Binding
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 14:1221-1227
ISSN:	0960-894X
Popis:	A variety of P4 motifs have been examined to increase the binding affinity and in vitro anticoagulant potency of our biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamide-based fXa inhibitors. Highly potent 2-naphthyl-P1 fXa inhibitors (K(i)or =2 nM) with improved in vitro anticoagulant activity (2xTGor =1 microM) and respectable pharmacokinetic properties have been discovered.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5398c5f418fd911780f5cf7f3549d9f1 https://doi.org/10.1016/j.bmcl.2003.12.053 Zobrazit plný text záznamu Full Text from ScienceDirect