Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease
Damalanka, Vishnu C. Kim, Yunjeong Kankanamalage, Anushka C. Galasiti Lushington, Gerald H. Mehzabeen, Nurjahan Battaile, Kevin P. Lovell, Scott Chang, Kyeong-Ok Groutas, William C.
Damalanka, Vishnu C.
Kim, Yunjeong
Kankanamalage, Anushka C. Galasiti
Lushington, Gerald H.
Mehzabeen, Nurjahan
Battaile, Kevin P.
Lovell, Scott
Chang, Kyeong-Ok
Groutas, William C.
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2017-02-15
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Macrocyclic inhibitors,Norovirus,3CL protease
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Damalanka, Vishnu C.; Kim, Yunjeong; Kankanamalage, Anushka C. Galasiti; Lushington, Gerald H.; Mehzabeen, Nurjahan; Battaile, Kevin P.; Lovell, Scott; Chang, Kyeong-Ok; Groutas, William C. 2017. Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease. European Journal of Medicinal Chemistry, vol. 127:pp 41–61
Abstract
Norovirus infections have a major impact on public health worldwide, yet there is a current dearth of norovirus-specific therapeutics and prophylactics. This report describes the discovery of a novel class of macrocyclic inhibitors of norovirus 3C-like protease, a cysteine protease that is essential for virus replication. SAR, structural, and biochemical studies were carried out to ascertain the effect of structure on pharmacological activity and permeability. Insights gained from these studies have laid a solid foundation for capitalizing on the therapeutic potential of the series of inhibitors described herein.
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Elsevier B.V.
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European Journal of Medicinal Chemistry;v.127
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0223-5234