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

Zhengqiang Wang; Robert Vince

doi:10.1016/j.bmcl.2008.01.025

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

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1293-6. doi: 10.1016/j.bmcl.2008.01.025. Epub 2008 Jan 11.

Authors

Zhengqiang Wang¹, Robert Vince

Affiliation

¹ Center for Drug Design, Academic Health Center, University of Minnesota, 516 Delaware St SE, Minneapolis, MN 55455, USA.

PMID: 18226894
DOI: 10.1016/j.bmcl.2008.01.025

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / chemistry
Anti-HIV Agents / pharmacology
HIV Integrase Inhibitors / chemical synthesis*
HIV Integrase Inhibitors / pharmacology
HIV Reverse Transcriptase / antagonists & inhibitors*
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / pharmacology
Quinolones / chemical synthesis
Quinolones / chemistry*
Quinolones / pharmacology
Reverse Transcriptase Inhibitors / chemical synthesis*
Reverse Transcriptase Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Anti-HIV Agents
HIV Integrase Inhibitors
Pyrimidines
Quinolones
Reverse Transcriptase Inhibitors
HIV Reverse Transcriptase