Identification of a potent and metabolically stable series of fluorinated diphenylpyridylethanamine-based cholesteryl ester transfer protein inhibitors

Autor:	James A. Johnson, Ramakrishna Seethala, Christine Huang, Michael M. Miller, David S. Taylor, Ji Jiang, Ruth R. Wexler, Mark E. Salvati, Jun Zhang, Xiaohong Yin, Yalei Liu, R. Michael Lawrence, Tatyana Zvyaga, David S. Nirschl, Lalgudi S. Harikrishnan, Tara L. Peterson, Michael A. Poss, Alice Ye A. Chen, Leonard P. Adam, Yufeng Wang, Muthoni G. Kamau
Rok vydání:	2012
Předmět:	Halogenation Pyridines Clinical Biochemistry Sterol O-acyltransferase Pharmaceutical Science Biochemistry chemistry.chemical_compound Mice Drug Discovery Cholesterylester transfer protein Moiety Animals Humans Urea Amines Molecular Biology CETP inhibitor biology Chemistry Organic Chemistry Reverse cholesterol transport In vitro Cholesterol Ester Transfer Proteins Rats biology.protein Molecular Medicine lipids (amino acids peptides and proteins)
Zdroj:	Bioorganicmedicinal chemistry letters. 22(20)
ISSN:	1464-3405
Popis:	A novel series of diphenylpyridylethanamine-based inhibitors of cholesteryl ester transfer protein is described. Optimization of the urea moiety, particularly by incorporation of fluorine, is explored to balance in vitro metabolic stability with CETP potency in the whole plasma assay.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e16e77fe68cebfc91bb03f93c0c149e1 https://pubmed.ncbi.nlm.nih.gov/22995620 Zobrazit plný text záznamu Full Text from ScienceDirect