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吡唑并[4,3 - d]嘧啶核苷。1 - β - D - 呋喃核糖基 - 3 - 甲基 - 6 - 取代 - 7H - 吡唑并[4,3 - d]嘧啶 - 7 - 酮的合成与抗病毒活性。

Pyrazolo[4,3-d]pyrimidine nucleosides. Synthesis and antiviral activity of 1-beta-D-ribofuranosyl-3-methyl-6-substituted-7H-pyrazolo[4,3-d]pyr imi din-7-ones.

作者信息

Baraldi P G, Simoni D, Periotto V, Manfredini S, Guarneri M, Manservigi R, Cassai E, Bertolasi V

出版信息

J Med Chem. 1984 Aug;27(8):986-90. doi: 10.1021/jm00374a009.

Abstract

N1 analogues of formycin B, with substituents at the 3 and 6 positions of the pyrazolo[4,3-d]pyrimidine moiety were synthesized by the direct SnCl4-catalyzed ribosylation method. The site of the glycosidic linkage and the anomeric configurations were established on the basis of X-ray crystallography, as well as 1H and 13C nuclear magnetic resonance spectroscopy. Preliminary results of the antiviral testing of these derivatives in vitro are described.

摘要

通过直接的SnCl4催化核糖基化方法合成了在吡唑并[4,3-d]嘧啶部分的3位和6位带有取代基的N1-间型霉素B类似物。基于X射线晶体学以及1H和13C核磁共振光谱确定了糖苷键的位置和端基构型。描述了这些衍生物体外抗病毒测试的初步结果。

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