Benfatti Fides, Cardillo Giuliana, Fabbroni Serena, Galzerano Patrizia, Gentilucci Luca, Juris Riccardo, Tolomelli Alessandra, Baiula Monica, Spartà Antonino, Spampinato Santi
Dipartimento di Chimica "G. Ciamician", Università di Bologna, Via Selmi 2, 40126 Bologna, Italy.
Bioorg Med Chem. 2007 Dec 1;15(23):7380-90. doi: 10.1016/j.bmc.2007.07.049. Epub 2007 Aug 22.
Small constrained non-peptidic molecules consisting of a polyfunctionalized rigid core, carrying appendages corresponding to arginine and aspartic acid side chains, have been recently reported to be promising for drug development. In this work, the 5,6-dihydropyridin-2-one was envisaged as a scaffold to turn into potential integrin ligands, introducing a carboxylic acid and a basic appendage. The synthesis and the antiadhesion activity of a small library of peptidomimetics capable to recognize alpha(v)beta(3) and alpha(5)beta(1) integrins has been herein reported.
最近有报道称，由多官能化刚性核心组成、带有对应于精氨酸和天冬氨酸侧链的附属基团的小分子受限非肽类分子在药物开发方面很有前景。在这项工作中，5,6 - 二氢吡啶 - 2 - 酮被设想为一种骨架，通过引入羧酸和碱性附属基团转化为潜在的整合素配体。本文报道了一个能够识别α(v)β(3)和α(5)β(1)整合素的拟肽小分子文库的合成及其抗黏附活性。
