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

✍ Scribed by Eric D. Jones; Nick Vandegraaff; Giang Le; Neil Choi; William Issa; Katherine Macfarlane; Neeranat Thienthong; Lisa J. Winfield; Jonathan A.V. Coates; Long Lu; Xinming Li; Xiao Feng; Changjiang Yu; David I. Rhodes; John J. Deadman

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 813 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.079

No coin nor oath required. For personal study only.

✦ Synopsis

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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