含二甲苯桥的环双啡肽类似物：合成、表征及生物学特性
Cyclic Biphalin Analogues Incorporating a Xylene Bridge: Synthesis, Characterization, and Biological Profile.
作者信息
Stefanucci Azzurra, Carotenuto Alfonso, Macedonio Giorgia, Novellino Ettore, Pieretti Stefano, Marzoli Francesca, Szűcs Edina, Erdei Anna I, Zádor Ferenc, Benyhe Sándor, Mollica Adriano
机构信息
Dipartimento di Farmacia, Università di Chieti-Pescara "G. d'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy.
Dipartimento di Farmacia, Università di Napoli "Federico II", Via D. Montesano, 49, 80131 Naples, Italy.
出版信息
ACS Med Chem Lett. 2017 Jul 12;8(8):858-863. doi: 10.1021/acsmedchemlett.7b00210. eCollection 2017 Aug 10.
Abstract
In this work we enhanced the ring lipophilicity of biphalin introducing a xylene moiety, thus obtaining three cyclic regioisomers. Novel compounds have similar activity as the parent compound, but one of these () shows a remarkable increase of antinociceptive effect. Nociception tests have disclosed its significant high potency and the more prolonged effect in eliciting analgesia, higher than that of biphalin and of the disulfide-bridge-containing analogue ().
摘要
在这项工作中，我们通过引入一个二甲苯部分来增强双啡肽的环亲脂性，从而获得了三种环状区域异构体。新型化合物具有与母体化合物相似的活性，但其中一种（）显示出抗伤害感受作用显著增强。伤害感受测试揭示了其显著的高效能以及在引发镇痛方面更持久的效果，高于双啡肽和含二硫键类似物（）。
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