基于螺环二酮哌嗪的 CCR5 拮抗剂：改善其药代动力学特征。
Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles.
机构信息
Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka 618-8585, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Jan 15;20(2):763-6. doi: 10.1016/j.bmcl.2009.11.018. Epub 2009 Nov 12.
Abstract
Spirodiketopiperazine-based CCR5 antagonists, showing improved pharmacokinetic profiles without reduction in antagonist activity, were designed and synthesized. We also demonstrate the anti-HIV activity of a representative compound 12, as measured in a p24 assay.
摘要
基于螺环二酮哌嗪的 CCR5 拮抗剂，在不降低拮抗活性的情况下显示出改善的药代动力学特征，被设计和合成。我们还展示了代表性化合物 12 的抗 HIV 活性，该活性通过 p24 测定来衡量。
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