Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus.
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ABSTRACT:
SUBMITTER: Mandadapu SR
PROVIDER: S-EPMC3750990 | biostudies-literature | 2013 Jul
REPOSITORIES: biostudies-literature
Publications
Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus.
Mandadapu Sivakoteswara Rao SR Weerawarna Pathum M PM Prior Allan M AM Uy Roxanne Adeline Z RA Aravapalli Sridhar S Alliston Kevin R KR Lushington Gerald H GH Kim Yunjeong Y Hua Duy H DH Chang Kyeong-Ok KO Groutas William C WC
Bioorganic & medicinal chemistry letters 20130516 13
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 5.1 μM, respectively. ...[more]
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