蘆平曲韋
化合物
蘆平曲韋(英語:Rupintrivir,也叫AG-7088、Rupinavir)是一種擬肽抗病毒藥物,可作為小核糖核酸病毒3C蛋白酶和3C樣蛋白酶抑制劑。[1][2][3]它是為治療鼻病毒而開發的,[4][5]隨後被研究用於治療其他病毒性疾病,包括由小核糖核酸病毒引起的疾病、[6][7]諾如病毒、[8]和冠狀病毒,例如SARS和COVID-19。[9][10]
臨床數據 | |
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商品名 | Rupintrivir |
法律規範狀態 | |
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識別資訊 | |
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CAS編號 | 223537-30-2 |
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化學資訊 | |
化學式 | C31H39FN4O7 |
摩爾質量 | 598.7 |
3D模型(JSmol) | |
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參見
參考文獻
- ^ Dragovich PS, Prins TJ, Zhou R, Webber SE, Marakovits JT, Fuhrman SA, et al. Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 4. Incorporation of P1 lactam moieties as L-glutamine replacements. Journal of Medicinal Chemistry. April 1999, 42 (7): 1213–24. PMID 10197965. doi:10.1021/jm9805384.
- ^ Santos MM, Moreira R. Michael acceptors as cysteine protease inhibitors. Mini Reviews in Medicinal Chemistry. October 2007, 7 (10): 1040–50. PMID 17979807. doi:10.2174/138955707782110105.
- ^ Yuan S, Fan K, Chen Z, Sun Y, Hou H, Zhu L. Structure of the HRV-C 3C-Rupintrivir Complex Provides New Insights for Inhibitor Design. Virologica Sinica. February 2020, 35 (4): 445–454. PMC 7462945 . PMID 32103448. doi:10.1007/s12250-020-00196-4.
- ^ Patick AK, Binford SL, Brothers MA, Jackson RL, Ford CE, Diem MD, et al. In vitro antiviral activity of AG7088, a potent inhibitor of human rhinovirus 3C protease. Antimicrobial Agents and Chemotherapy. October 1999, 43 (10): 2444–50. PMC 89498 . PMID 10508022. doi:10.1128/AAC.43.10.2444.
- ^ Jensen LM, Walker EJ, Jans DA, Ghildyal R. Proteases of human rhinovirus: role in infection. Rhinoviruses. Methods in Molecular Biology 1221. 2015: 129–41. ISBN 978-1-4939-1570-5. PMID 25261311. doi:10.1007/978-1-4939-1571-2_10.
- ^ Barnard DL. Current status of anti-picornavirus therapies. Current Pharmaceutical Design. 2006, 12 (11): 1379–90. PMID 16611122. doi:10.2174/138161206776361129.
- ^ De Palma AM, Vliegen I, De Clercq E, Neyts J. Selective inhibitors of picornavirus replication. Medicinal Research Reviews. November 2008, 28 (6): 823–84. PMID 18381747. S2CID 1575335. doi:10.1002/med.20125.
- ^ Rocha-Pereira J, Nascimento MS, Ma Q, Hilgenfeld R, Neyts J, Jochmans D. The enterovirus protease inhibitor rupintrivir exerts cross-genotypic anti-norovirus activity and clears cells from the norovirus replicon. Antimicrobial Agents and Chemotherapy. August 2014, 58 (8): 4675–81. PMC 4136040 . PMID 24890597. doi:10.1128/AAC.02546-13.
- ^ Anand K, Ziebuhr J, Wadhwani P, Mesters JR, Hilgenfeld R. Coronavirus main proteinase (3CLpro) structure: basis for design of anti-SARS drugs. Science. June 2003, 300 (5626): 1763–7. Bibcode:2003Sci...300.1763A. PMID 12746549. doi:10.1126/science.1085658 .
- ^ 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 .