Ottanà Rosaria, Maccari Rosanna, Giglio Marco, Del Corso Antonella, Cappiello Mario, Mura Umberto, Cosconati Sandro, Marinelli Luciana, Novellino Ettore, Sartini Stefania, La Motta Concettina, Da Settimo Federico
Dipartimento Farmaco-chimico, Università di Messina, Polo Universitario Annunziata, 98168 Messina, Italy.
Eur J Med Chem. 2011 Jul;46(7):2797-806. doi: 10.1016/j.ejmech.2011.03.068. Epub 2011 Apr 8.
In continuing the search for more effective 5-arylidene-4-thiazolidinones as aldose reductase inhibitors, a new set of suitably substituted compounds (4, 5 and 8) was explored. Acetic acids 5, particularly 5a and 5h, proved to be interesting inhibitors of the enzyme as well as excellent antioxidant agents that are potentially able to counteract the oxidative stress associated with both diabetic complications as well as other pathologies. Molecular docking experiments supported SAR studies.
在继续寻找更有效的5-亚芳基-4-噻唑烷酮作为醛糖还原酶抑制剂的过程中，研究了一组新的适当取代的化合物（4、5和8）。乙酸5，特别是5a和5h，被证明是该酶的有趣抑制剂，也是潜在能够对抗与糖尿病并发症以及其他病症相关的氧化应激的优秀抗氧化剂。分子对接实验支持了构效关系研究。
