Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir. Issue 17 (1st September 2020)

• Record Type: Journal Article
• Authors: Clausen, Dane J.; Liu, Jian; Yu, Wensheng; Duffy, Joseph L.; Chung, Christine C.; Myers, Robert W.; Klein, Daniel J.; Fells, James; Holloway, Kate; Wu, Jin; Wu, Guoxin; Howell, Bonnie J.; Barnard, Richard J.O.; Kozlowski, Joseph
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 17(2020)
• Publication Date: 2020-09-01
• Subjects: Medicinal chemistry -- HDAC -- HIV -- Latent reservoir -- X-ray structure -- SAR analysis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2020.127367
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.