Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 2CL Protease
Damalanka, Vishnu C.
Alliston, Kevin R.
Weerawarna, Pathum M.
Kankanamalage, Anushka C. Galasiti
Lushington, Gerald H.
Battaile, Kevin P.
Groutas, William C.
American Chemical Society
Scholarly/refereed, author accepted manuscript
This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://dx.doi.org/10.1021/acs.jmedchem.5b01464.
MetadataShow full item record
Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or prophylaxis of norovirus infections. Norovirus 3CL protease plays a vital role in viral replication by generating structural and nonstructural proteins via the cleavage of the viral polyprotein. Thus, molecules that inhibit the viral protease may have potential therapeutic value. We describe herein the structure-based design, synthesis, and in vitro and cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of norovirus 3CL protease.
Damalanka, V. C., Kim, Y., Alliston, K. R., Weerawarna, P. M., Galasiti Kankanamalage, A. C., Lushington, G. H., … Groutas, W. C. (2016). Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease. Journal of Medicinal Chemistry, 59(5), 1899–1913. http://doi.org/10.1021/acs.jmedchem.5b01464
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