Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses

Giang Le, Nick Vandegraaff, David I. Rhodes, Eric D. Jones, Jonathan A V Coates, Long Lu, Xinming Li, Changjiang Yu, Xiao Feng, John J. Deadman

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22 Citations (Scopus)


A series of novel HIV integrase inhibitors active against rategravir resistant strains are reported. Initial SAR studies revealed that activities against wild-type virus were successfully maintained at single digit nanomolar level with a wide range of substitutions. However, inclusion of nitrogen-based cyclic substitutions was crucial for achieving potency against mutant viruses. Several compounds with excellent activities against wild-type virus as well as against the viruses with the mutations Q148H/G140S or N155H/E92Q were reported.

Original languageEnglish
Pages (from-to)5013-5018
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number17
Publication statusPublished - 1 Sept 2010
Externally publishedYes


  • HIV
  • Inhibitor
  • Integrase
  • Mutant virus
  • NHEQ
  • QHGS
  • Synthesis

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