Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus

The design, synthesis, and in vitro inhibitory activity of the first series of macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus, are reported. The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases o...

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Published in	Bioorganic & medicinal chemistry letters Vol. 23; no. 13; pp. 3709 - 3712
Main Authors	Mandadapu, Sivakoteswara Rao, Weerawarna, Pathum M., Prior, Allan M., Uy, Roxanne Adeline Z., Aravapalli, Sridhar, Alliston, Kevin R., Lushington, Gerald H., Kim, Yunjeong, Hua, Duy H., Chang, Kyeong-Ok, Groutas, William C.
Format	Journal Article
Language	English
Published	OXFORD Elsevier Ltd 01.07.2013 Elsevier
Subjects	3C and 3CL proteases Chemistry Chemistry, Medicinal Chemistry, Organic Coronavirus Coronavirus - enzymology Dose-Response Relationship, Drug Drug Design Enterovirus in vitro studies Life Sciences & Biomedicine Macrocyclic Compounds - chemical synthesis Macrocyclic Compounds - chemistry Macrocyclic Compounds - pharmacology Macrocyclic inhibitors Models, Molecular Molecular Conformation Norovirus Norovirus - enzymology Peptide Hydrolases - metabolism Pharmacology & Pharmacy Physical Sciences Picornaviridae - enzymology Picornavirus Picornavirus-like supercluster pathogens Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology proteinases SARS coronavirus Science & Technology Severe acute respiratory syndrome coronavirus Structure-Activity Relationship Macrocyclic inhibitors 3C and 3CL proteases Picornavirus-like supercluster pathogens DRUG NORWALK-VIRUS ENTEROVIRUS 71 CYSTEINE PEPTIDE SUBSTRATE-SPECIFICITY REPLICATION POTENT INHIBITION RUPINTRIVIR STRUCTURE-BASED DESIGN
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Summary:	The design, synthesis, and in vitro inhibitory activity of the first series of macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus, are reported. The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus are reported. The in vitro inhibitory activity (50% effective concentration) of the macrocyclic inhibitor toward enterovirus 3C protease (CVB3 Nancy strain), and coronavirus (SARS-CoV) and norovirus 3C-like proteases, was determined to be 1.8, 15.5 and 5.1μM, respectively.
Bibliography:	http://dx.doi.org/10.1016/j.bmcl.2013.05.021 NIH RePORTER ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-1 content type line 23 These authors contributed equally to this work.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2013.05.021