7-氧代-4,7-二氢噻吩并[3,2-b]吡啶-6-甲酰胺：一类新型高效人巨细胞病毒DNA聚合酶抑制剂的合成与生物活性
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
作者信息
Larsen Scott D, Zhang Zhijun, DiPaolo Brian A, Manninen Peter R, Rohrer Douglas C, Hageman Michael J, Hopkins Todd A, Knechtel Mary L, Oien Nancee L, Rush Bob D, Schwende Francis J, Stefanski Kevin J, Wieber Janet L, Wilkinson Karen F, Zamora Kathyrn M, Wathen Michael W, Brideau Roger J
机构信息
Pfizer Global Research and Development, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3840-4. doi: 10.1016/j.bmcl.2007.05.010. Epub 2007 May 10.
We report a new class of non-nucleoside antivirals, the 7-oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides, some of which possess remarkable potency versus a broad spectrum of herpesvirus DNA polymerases and excellent selectivity compared to human DNA polymerases. A critical factor in the level of activity is hypothesized to be conformational restriction of the key 2-aryl-2-hydroxyethylamine sidechain by an adjacent methyl group.
我们报道了一类新型非核苷抗病毒药物，即7-氧代-4,7-二氢噻吩并[3,2-b]吡啶-6-甲酰胺，其中一些对多种疱疹病毒DNA聚合酶具有显著活性，并且与人DNA聚合酶相比具有出色的选择性。据推测，活性水平的一个关键因素是相邻甲基对关键的2-芳基-2-羟乙胺侧链的构象限制。
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