Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.
Eur J Med Chem. 2012 Jan;47(1):59-64. doi: 10.1016/j.ejmech.2011.10.019. Epub 2011 Oct 20.
An optimization campaign focused on improving pharmacological activity and physicochemical properties of a recently-identified class of cyclosulfamide-based norovirus inhibitors has been carried out. Dimeric compound 4 was found to be a ∼10-fold more potent norovirus inhibitor (ED(50) 0.4 μM) compared to the original hit, however, isonipecotic acid ester derivatives 7e and 10a were shown to have superior therapeutic indices.
一项旨在改善最近发现的一类基于环硫酰胺的诺如病毒抑制剂的药理活性和物理化学性质的优化活动已经开展。二聚体化合物 4 被发现比原始命中物具有约 10 倍更高的诺如病毒抑制活性（ED(50)0.4μM），然而，异哌啶酸酯衍生物 7e 和 10a 显示出更好的治疗指数。
