Synthesis, Crystal Structure, Structure−Activity Relationships, and Antiviral Activity of a Potent SARS Coronavirus 3CL Protease Inhibitor
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Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors.
N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC50 values ranging from 0.95 to 17.50 microM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavir...
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(1999). 32. C. L. Colby, J. R. Duhamel, M. E. Goldberg, Cereb. Cortex 5, 470 (1995). 33. K. Nakamura, C. L. Colby, Proc. Natl. Acad. Sci. U.S.A. 99, 4026 (2002). 34. S. Ben Hamed, J. R. Duhamel, Exp. Brain Res. 142, 512 (1998). 35. B. Gaymard, C. J. Ploner, S. Rivaud, A. I. Vermersch, C. Pierrot-Deseilligny, Exp. Brain Res. 123, 159 (1998). 36. D. C. Somers, S. B. Nelson, M. Sur, J. Neurosci. 1...
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The severe acute respiratory syndrome (SARS) coronavirus 3CL protease is an attractive target for the development of anti-SARS drugs. In this paper, cinanserin (1) analogs were synthesized and tested for the inhibitory activities against SARS-coronavirus (CoV) 3CL protease by fluorescence resonance energy transfer (FRET) assay. Four analogs show significant activities, especially compound 26 wi...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2006
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm0603926