3CLpro-1
3CLpro-1是一種與蘆平曲韋相關的抗病毒藥物,作為3C樣蛋白酶抑制劑,最初開發用於治療人類腸病毒71型。它是作為病毒酶3C樣蛋白酶抑制劑開發的眾多化合物中最有效的一種蛋白酶,體外IC50為200nM。它還顯示出對SARS和MERS等冠狀病毒疾病的活性,並且正在研究作為病毒性疾病COVID-19的潛在治療劑。病毒性疾病COVID-19的治療劑。[1][2][3][4][5][6][7]
臨床資料 | |
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商品名 | 3CLpro-1 |
法律規範狀態 | |
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識別資訊 | |
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CAS號 | 2409054-43-7 |
PubChem CID | |
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化學資訊 | |
化學式 | C25H25ClFN3O4 |
摩爾質量 | 640.8 |
3D模型(JSmol) | |
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另見
參考資料
- ^ Kuo CJ, Shie JJ, Fang JM, Yen GR, Hsu JT, Liu HG, et al. Design, synthesis, and evaluation of 3C protease inhibitors as anti-enterovirus 71 agents. Bioorganic & Medicinal Chemistry. August 2008, 16 (15): 7388–98. PMC 7125518 . PMID 18583140. doi:10.1016/j.bmc.2008.06.015.
- ^ Zhou Y, Vedantham P, Lu K, Agudelo J, Carrion R, Nunneley JW, et al. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Research. April 2015, 116: 76–84. PMC 4774534 . PMID 25666761. doi:10.1016/j.antiviral.2015.01.011 .
- ^ Kumar V, Shin JS, Shie JJ, Ku KB, Kim C, Go YY, et al. Identification and Evaluation of Potent Middle East Respiratory Syndrome Coronavirus (MERS-CoV) 3CL Pro Inhibitors. Antiviral Research. May 2017, 141: 101–106. PMC 7113684 . PMID 28216367. doi:10.1016/j.antiviral.2017.02.007 .
- ^ Liu C, Zhou Q, Li Y, Garner LV, Watkins SP, Carter LJ, et al. Research and Development on Therapeutic Agents and Vaccines for COVID-19 and Related Human Coronavirus Diseases. ACS Central Science. 2020, 6 (3): 315–331. PMC 7094090 . PMID 32226821. doi:10.1021/acscentsci.0c00272 .
- ^ Morse JS, Lalonde T, Xu S, Liu WR. Learning from the Past: Possible Urgent Prevention and Treatment Options for Severe Acute Respiratory Infections Caused by 2019-nCoV. ChemBioChem. March 2020, 21 (5): 730–738. PMC 7162020 . PMID 32022370. doi:10.1002/cbic.202000047 .
- ^ Zhang L, Lin D, Kusov Y, Nian Y, Ma Q, Wang J, et al. α-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment. Journal of Medicinal Chemistry. February 2020, 63 (9): 4562–4578. PMC 7098070 . PMID 32045235. doi:10.1021/acs.jmedchem.9b01828 .
- ^ Zhang L, Lin D, Sun X, Curth U, Drosten C, Sauerhering L, et al. Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors. Science. March 2020, 368 (6489): 409–412. PMC 7164518 . PMID 32198291. doi:10.1126/science.abb3405 .