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Design, synthesis, and evaluation of inhibitors for severe acute respiratory syndrome 3C-like protease based on phthalhydrazide ketones or heteroaromatic esters

J Zhang, HI Pettersson, C Huitema, C Niu…

文献索引:Zhang, Jianmin; Pettersson, Hanna I.; Huitema, Carly; Niu, Chunying; Yin, Jiang; James, Michael N. G.; Eltis, Lindsay D.; Vederas, John C. Journal of Medicinal Chemistry, 2007 , vol. 50, # 8 p. 1850 - 1864

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被引用次数: 34

摘要

The 3C-like protease (3CLpro), which controls the severe acute respiratory syndrome (SARS) coronavirus replication, has been identified as a potential target for drug design in the treatment of SARS. A series of tetrapeptide phthalhydrazide ketones, pyridinyl esters, and their analogs have been designed, synthesized, and evaluated as potential SARS 3CLpro inhibitors. Some pyridinyl esters are identified as very potent inhibitors, with IC50 ...