[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring

Autor:	Terry P. Kenakin, Robert G. Ferris, Christopher Joseph Aquino, Pat Wheelan, Michael Youngman, Chris Watson, Cecilia S. Koble, Maosheng Duan, Wieslaw M. Kazmierski
Rok vydání:	2009
Předmět:	Receptors CCR5 Anti-HIV Agents Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Human immunodeficiency virus (HIV) Pharmaceutical Science HIV Infections CHO Cells Ring (chemistry) medicine.disease_cause Biochemistry Chemical synthesis Inhibitory Concentration 50 chemistry.chemical_compound Cricetulus Piperidines In vivo Cricetinae Drug Discovery medicine Animals Inhibitory concentration 50 Derivatization Molecular Biology Organic Chemistry Protein Structure Tertiary Rats chemistry Drug Design CCR5 Receptor Antagonists HIV-1 Molecular Medicine Amine gas treating Piperidine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:1610-1613
ISSN:	0960-894X
Popis:	Several series of CCR5 antagonists have been discovered by derivatization at the N-terminal of the piperidine ring of the core template 2. Some derivatives exhibited potent inhibition against HIV-1infection. The pharmacokinetic properties of the lead compounds 11a, 14a, 15b, and 16b have been evaluated in vivo.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b95251eb83cd30c70b43dd2a152648fc https://doi.org/10.1016/j.bmcl.2009.02.014 Zobrazit plný text záznamu Full Text from ScienceDirect