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Bicyclic Hydroxy-1H-pyrrolopyridine-trione Containing HIV-1 Integrase Inhibitors

✍ Scribed by Xue Zhi Zhao; Kasthuraiah Maddali; Mathieu Metifiot; Steven J. Smith; B. Christie Vu; Christophe Marchand; Stephen H. Hughes; Yves Pommier; Terrence R. Burke Jr


Book ID
111369095
Publisher
John Wiley and Sons
Year
2011
Tongue
English
Weight
418 KB
Volume
79
Category
Article
ISSN
1747-0277

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Design of a series of bicyclic HIV-1 int
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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.