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Updated: Jun 3, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
3-Hydroxypyrimidine-2,4-diones as an inhibitor scaffold of HIV integrase
Jing Tang1, Kasthuraiah Maddali, Mathieu Metifiot
1Center for Drug Design, Academic Health Center, University of Minnesota, Minneapolis, Minnesota 55455, United States.
Abstract:
Integrase (IN) represents a clinically validated target for the development of antivirals against human immunodeficiency virus (HIV). Inhibitors with a novel structure core are essential for combating resistance associated with known IN inhibitors (INIs). We have previously disclosed a novel dual inhibitor scaffold of HIV IN and reverse transcriptase (RT). Here we report the complete structure-activity relationship (SAR), molecular modeling, and resistance profile of this inhibitor type on IN inhibition. These studies support an antiviral mechanism of dual inhibition against both IN and RT and validate 3-hydroxypyrimidine-2,4-diones as an IN inhibitor scaffold.
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