Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: A series of potent NS3 protease inhibitors for the treatment of hepatitis C virus. Issue 3 (1st February 2017)

• Record Type: Journal Article
• Authors: Wang, Alan Xiangdong; Chen, Jie; Zhao, Qian; Sun, Li-Qiang; Friborg, Jacques; Yu, Fei; Hernandez, Dennis; Good, Andrew C.; Klei, Herbert E.; Rajamani, Ramkumar; Mosure, Kathy; Knipe, Jay O.; Li, Danshi; Zhu, Jialong; Levesque, Paul C.; McPhee, Fiona; Meanwell, Nicholas A.; Scola, Paul M.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 3(2017)
• Page Start: 590
• Page End: 596
• Publication Date: 2017-02-01
• Subjects: HCV NS3/4A serine protease inhibitors -- Tripeptide acylsulfonamides -- C4 aryl, C4 hydroxy-proline -- Potent and orally bioavailable -- Cardiovascular profiles; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.12.013
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: The design and synthesis of a series of tripeptide acylsulfonamides as potent inhibitors of the HCV NS3/4A serine protease is described. These analogues house a C4 aryl, C4 hydroxy-proline at the S2 position of the tripeptide scaffold. Information relating to structure-activity relationships as well as the pharmacokinetic and cardiovascular profiles of these analogues is provided.