Synthesis of pyrimidine and quinolone conjugates as a scaffold for dual inhibitors of HIV reverse transcriptase and integrase

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Abstract

A series of conjugates combining a pyrimidine and a quinolone moiety were designed and synthesized. The assay results show that these compounds demonstrate both anti-RT activity and anti-IN activity and therefore provide a useful scaffold for identifying inhibitors with balanced dual activities.

Original languageEnglish (US)
Pages (from-to)1293-1296
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number4
DOIs
StatePublished - Feb 15 2008

Bibliographical note

Funding Information:
This research was supported by the Center for Drug Design at the University of Minnesota. We thank Dr. Eric Bennett for discussion, Dr. Christine Salomon for IN assay, and Christine Dreis for RT assay. We also thank Roger Ptak at Southern Research Institute for cell-based assay and Dr. Robert Craigie of NIH for the integrase plasmid.

Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.

Keywords

  • Dual inhibitor
  • HIV
  • Integrase
  • Rational design
  • Reverse transcriptase

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