Discovery of hydroxy pyrimidine Factor IXa inhibitors

Autor:	Charles Lee Jayne, Santhosh Neelamkavil, Alan Hruza, Richard N. Ingram, Samuel Chackalamannil, Mariappan V. Chelliah, Keith Eagen, Teresa Andreani, William J. Greenlee, Kartik M. Keertikar, Steve Fried, Brian Hawes, Yan Xia, Zhuyan Guo, Michael P. Dwyer, Tin-Yau Chan, Paul Reichert, Martin C. Clasby
Rok vydání:	2020
Předmět:	Pyrimidine Stereochemistry Clinical Biochemistry Pharmaceutical Science 01 natural sciences Biochemistry Factor IXa chemistry.chemical_compound Structure-Activity Relationship In vivo Drug Discovery Structure–activity relationship Humans Molecular Biology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry Plasma levels 0104 chemical sciences 010404 medicinal & biomolecular chemistry Pyrimidines Molecular Medicine Selectivity Factor Xa Inhibitors
Zdroj:	Bioorganicmedicinal chemistry letters. 30(15)
ISSN:	1464-3405
Popis:	The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described. Increased selectivity over Factor Xa inhibition was achieved through SAR expansion of the P1 element. Select compounds were evaluated in vivo to assess their plasma levels in rat.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c095f071ef48433855bcea54d91788f5 https://pubmed.ncbi.nlm.nih.gov/32527459 Zobrazit plný text záznamu Full Text from ScienceDirect