Potent inhibition of norovirus 3CL protease by peptidyl α-ketoamides and α-ketoheterocycles.
A series of structurally-diverse α-ketoamides and α-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.
Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.
Sivakoteswara Rao
SR
Mandadapu
Pathum M
PM
Weerawarna
Mallikarjuna Reddy
MR
Gunnam
Kevin R
KR
Alliston
Gerald H
GH
Lushington
Yunjeong
Y
Kim
Kyeong-Ok
KO
Chang
William C
WC
Groutas
D000577:Amides / Q000737:chemistry* / Q000494:pharmacology; D003546:Cysteine Endopeptidases / Q000737:chemistry* / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D029322:Norovirus / Q000187:drug effects / Q000201:enzymology*; D010455:Peptides / Q000737:chemistry*; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000577:Amides; D006571:Heterocyclic Compounds; D010455:Peptides; D011480:Protease Inhibitors; D003546:Cysteine Endopeptidases