点击化学衍生的苯并[d]异噻唑-3(2H)-酮衍生物对登革热病毒和西尼罗河病毒蛋白酶的抑制作用。
Inhibition of Dengue virus and West Nile virus proteases by click chemistry-derived benz[d]isothiazol-3(2H)-one derivatives.
机构信息
Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.
出版信息
Bioorg Med Chem. 2012 Feb 1;20(3):1213-21. doi: 10.1016/j.bmc.2011.12.047. Epub 2011 Dec 30.
Abstract
Two click chemistry-derived focused libraries based on the benz[d]isothiazol-3(2H)-one scaffold were synthesized and screened against Dengue virus and West Nile virus NS2B-NS3 proteases. Several compounds (4l, 7j-n) displayed noteworthy inhibitory activity toward Dengue virus NS2B-NS3 protease in the absence and presence of added detergent. These compounds could potentially serve as a launching pad for a hit-to-lead optimization campaign.
摘要
基于苯并[d]异噻唑-3(2H)-酮骨架，合成了两个点击化学衍生的靶向文库，并对登革热病毒和西尼罗河病毒 NS2B-NS3 蛋白酶进行了筛选。一些化合物（4l、7j-n）在有无添加去污剂的情况下对登革热病毒 NS2B-NS3 蛋白酶表现出显著的抑制活性。这些化合物可能成为从命中到先导优化的一个起点。
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