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区域选择性合成 6-取代-2-氨基-5-溴-4(3H)-嘧啶酮及其抗病毒活性评价。

Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity.

机构信息

Department of Chemistry, UGC-Centre of Advance Study-I, Guru Nanak Dev University, Amritsar 143005, India.

出版信息

Eur J Med Chem. 2013 Sep;67:428-33. doi: 10.1016/j.ejmech.2013.06.036. Epub 2013 Jul 5.

DOI:10.1016/j.ejmech.2013.06.036
PMID:23911856
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7127258/
Abstract

A series of 2-amino-5-bromo-4(3H)-pyrimidinone derivatives bearing different substituents at the C-6 position were synthesized using a highly regioselective lithiation-substitution protocol, and the effect of structural variation at the C-6 position on their antiviral activity in cell culture was evaluated. Although some of the derivatives were found to be active against various virus strains, they were effective only close to their toxicity threshold.

摘要

一系列在 C-6 位带有不同取代基的 2-氨基-5-溴-4(3H)-嘧啶酮衍生物是通过高度区域选择性的锂化取代反应合成的，并评估了 C-6 位结构变化对其在细胞培养中的抗病毒活性的影响。尽管一些衍生物对各种病毒株具有活性，但它们只有在接近毒性阈值时才有效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b61e/7127258/ef21e2e1c078/sc2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b61e/7127258/c1eb70b7318a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b61e/7127258/3b073e193845/sc1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b61e/7127258/ef21e2e1c078/sc2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b61e/7127258/c1eb70b7318a/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b61e/7127258/3b073e193845/sc1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b61e/7127258/ef21e2e1c078/sc2.jpg

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