| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370795 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
A potent and novel class of product-like inhibitors of the HCV NS3 protease was discovered by employing a phosphinic acid as a carboxylate isostere. The replicon activity and pharmacokinetic profile of this series of compounds was optimized by exploring the substitution of the phosphinic acid, as well as conformationally constraining these compounds through macrocyclization. The syntheses and preliminary biological evaluation of these phosphinic acids is described.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Michael O. Clarke, Xiaowu Chen, Aesop Cho, William E. Delaney IV, Edward Doerffler, Maria Fardis, Mingzhe Ji, Michael Mertzman, Rowchanak Pakdaman, Hyun-Jun Pyun, Tanisha Rowe, Cheng Y. Yang, X. Christopher Sheng, Choung U. Kim,