对单纯疱疹病毒（HSV）和多种RNA病毒具有抗病毒活性的5-异恶唑-5-基-2'-脱氧尿苷的合成。
Synthesis of 5-isoxazol-5-yl-2'-deoxyuridines exhibiting antiviral activity against HSV and several RNA viruses.
作者信息
Lee Yoon-Suk, Park Sun Min, Kim Byeang Hyean
机构信息
Department of Chemistry, BK School of Molecular Science, Pohang University of Science and Technology, Pohang 790-784, South Korea.
出版信息
Bioorg Med Chem Lett. 2009 Feb 15;19(4):1126-8. doi: 10.1016/j.bmcl.2008.12.103. Epub 2008 Dec 31.
This paper describes a simple method for synthesizing a small library of 5-isoxazol-5-yl-2'-deoxyuridines from 5-iodo-2'-deoxyuridine. Nitrile oxides were generated in situ from oximes using a commercial bleaching agent; their cycloaddition with 5-ethynyl-2'-deoxyuridine yielded isoxazoles possessing activity against herpes simplex viruses 1 and 2, Encephalomyocarditis virus, Coxsackie B3, and vesicular stomatitis virus; these isoxazoles were, however, inactive against corona virus, influenza virus, and HIV.
本文描述了一种从5-碘-2'-脱氧尿苷合成一个小型5-异恶唑-5-基-2'-脱氧尿苷库的简单方法。使用市售漂白剂由肟原位生成腈氧化物；它们与5-乙炔基-2'-脱氧尿苷的环加成反应产生了对单纯疱疹病毒1型和2型、脑心肌炎病毒、柯萨奇B3病毒和水疱性口炎病毒具有活性的异恶唑；然而，这些异恶唑对冠状病毒、流感病毒和HIV无活性。
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