Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold

HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC 50 of 3 nM against wild type HIV infected T-cells.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-10, Vol.20 (19), p.5913-5917
Hauptverfasser:	Jones, Eric D., Vandegraaff, Nick, Le, Giang, Choi, Neil, Issa, William, Macfarlane, Katherine, Thienthong, Neeranat, Winfield, Lisa J., Coates, Jonathan A.V., Lu, Long, Li, Xinming, Feng, Xiao, Yu, Changjiang, Rhodes, David I., Deadman, John J.
Format:	Artikel
Sprache:	eng
Schlagworte:	3-Hydroxy-pyrido[12- a]pyrimidin-4-one Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Biological and medical sciences Bridged Bicyclo Compounds - chemical synthesis Bridged Bicyclo Compounds - chemistry Bridged Bicyclo Compounds - pharmacology Drug Design HIV Integrase - chemistry HIV Integrase - metabolism HIV Integrase Inhibitors - chemical synthesis HIV Integrase Inhibitors - chemistry HIV Integrase Inhibitors - pharmacology HIV-1 - drug effects Humans Inhibitor Integrase Medical sciences Pharmacology. Drug treatments Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Structure-Activity Relationship Synthesis T-Lymphocytes - virology
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Beschreibung
Zusammenfassung:	HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC 50 of 3 nM against wild type HIV infected T-cells.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.07.079