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

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

Research output: Contribution to journalArticleResearchpeer-review

37 Citations (Scopus)

Abstract

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 EC50 of 3 nM against wild type HIV infected T-cells.

Original languageEnglish
Pages (from-to)5913-5917
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number19
DOIs
Publication statusPublished - 1 Oct 2010
Externally publishedYes

Keywords

  • 3-Hydroxy-pyrido[12-a]pyrimidin-4-one
  • Inhibitor
  • Integrase
  • Synthesis

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