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Updated: Jun 18, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Solid phase synthesis of novel pyrrolidinedione analogs as potent HIV-1 integrase inhibitors
Annapurna Pendri1, Timothy L Troyer, Michael J Sofia
1Bristol-Myers Squibb Research and Development, Wallingford, Connecticut 06492, USA. annapurna.pendri@bms.com
Abstract:
A novel series of HIV-1 integrase inhibitors were identified from a 100 member (4R(1) x 5R(2) x 5R(3)) library of pyrrolidinedione amides. A solid-phase route was developed which facilitates the simultaneous variation at R(1), R(2), and R(3) of the pyrrolidinedione scaffold. The resulting library samples were assayed for HIV-1 integrase activity and analyzed to determine the R(1), R(2), and R(3) reagent contributions towards the activity.
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