Potent inhibition of norovirus 3CL protease by peptidyl α-ketoamides and α-ketoheterocycles

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:22

Article

Mandadapu, Sivakoteswara Rao¹  Weerawarna, Pathum M.¹  Gunnam, Mallikarjuna Reddy¹  Alliston, Kevin R.¹  Lushington, Gerald H.²  Kim, Yunjeong³  Chang, Kyeong-Ok³  Groutas, William C.¹ 

[1] Wichita State Univ, Dept Chem, Wichita, KS 67260 USA

[2] Univ Kansas, Mol Graph & Modeling Lab, Lawrence, KS 66045 USA

[3] Kansas State Univ, Dept Diagnost Med Pathobiol, Coll Vet Med, Manhattan, KS 66506 USA

关键词: alpha-Ketoamides;    Norovirus 3CL protease;    Norovirus;    Transition state inhibitors;   

DOI  :  10.1016/j.bmcl.2012.05.055

来源: Elsevier

【 摘 要 】

A series of structurally-diverse alpha-ketoamides and alpha-ketoheterocycles was synthesized and subsequently investigated for inhibitory activity against norovirus 3CL protease in vitro, as well as anti-norovirus activity in a cell-based replicon system. The synthesized compounds were found to inhibit norovirus 3CL protease in vitro and to also exhibit potent anti-norovirus activity in a cell-based replicon system. (C) 2012 Elsevier Ltd. All rights reserved.

【 授权许可】

Free