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High Throughput In Vitro Assessment of Latency Reversing Agents on HIV Transcription and Splicing
Published on: January 22, 2019
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Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir
Dane J Clausen1, Jian Liu1, Wensheng Yu1
1Merck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Bioorganic & Medicinal Chemistry Letters
|August 3, 2020
Abstract:
The synthesis and SAR development of a trisubstituted imidazole HDAC inhibitor is described. The compounds were synthesized with high diastereocontrol by leveraging Ellman sulfinyl imine chemistry. Structural elucidation provided insight into binding mode and supported design rational. Pharmacokinetic properties of lead compounds were determined.
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