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Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators

โœ Scribed by Giang Le; Nick Vandegraaff; David I. Rhodes; Eric D. Jones; Jonathan A.V. Coates; Neeranat Thienthong; Lisa J. Winfield; Long Lu; Xinming Li; Changjiang Yu; Xiao Feng; John J. Deadman


Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
781 KB
Volume
20
Category
Article
ISSN
0960-894X

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Design of a series of bicyclic HIV-1 int
โœ Eric D. Jones; Nick Vandegraaff; Giang Le; Neil Choi; William Issa; Katherine Ma ๐Ÿ“‚ Article ๐Ÿ“… 2010 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 813 KB

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.