The design and discovery of novel amide CCR5 antagonists

Autor:	Gemma C. Parsons, Peter T. Stephenson, Michelle Y. Platts, Barber Christopher Gordon, Blanda Luzia Christa Stammen, David C. Pryde, David Ellis, David W. Gordon, Helen J. Mason, Rachel L. Eastwood, Catherine Burt, Donald Stuart Middleton, David Bachelor, Martin Corless, Keith Statham, Anthony Wood, Wolfgang Klute, Kerry A. Paradowski, David C. Blakemore, David R. Fenwick
Rok vydání:	2009
Předmět:	ERG1 Potassium Channel Anti-HIV Agents Stereochemistry Clinical Biochemistry Human immunodeficiency virus (HIV) Pharmaceutical Science CCR5 receptor antagonist medicine.disease_cause Biochemistry Structure-Activity Relationship chemistry.chemical_compound Piperidines Amide Drug Discovery medicine Combinatorial Chemistry Techniques Humans Structure–activity relationship Molecular Biology Primary (chemistry) Molecular Structure Drug discovery Organic Chemistry Amides Combinatorial chemistry Ether-A-Go-Go Potassium Channels chemistry Drug Design CCR5 Receptor Antagonists HIV-1 Microsomes Liver Molecular Medicine Piperidine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:1084-1088
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2009.01.012
Popis:	The synthesis of a range of novel amine-containing structures and their primary potency as inhibitors of HIV-1 fusion via blocking of the CCR5 receptor is described. The development of the medicinal chemistry strategy and SAR's which led to the identification of the piperidine amide compounds 33 and 36 as excellent leads for further evaluation is described, along with key physicochemical data which highlighted their lead potential.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::619f831846652fe35ab392fac3f0b7c7 https://doi.org/10.1016/j.bmcl.2009.01.012 Zobrazit plný text záznamu Full Text from ScienceDirect