(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators
作者:Marouan Rami、Jean-Yves Winum、Claudiu T. Supuran、Patricia Melnyk、Saïd Yous
DOI:10.1080/14756366.2018.1543292
日期:2019.1.1
Abstract Using histamine as lead molecule, a library of (hetero)aryl substituted thiazol-2,4-yl derivatives incorporating pyridine as proton shuttling moiety were obtained and investigated as activators of human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I, II, VII and XIV. Some derivatives displayed good activating and selectivity profiles. This study provides an interesting opportunity to study
抽象的 使用组胺作为前导分子,获得了以吡啶作为质子穿梭部分的(杂)芳基取代的噻唑-2,4-基衍生物文库,并作为人碳酸酐酶(CA,EC 4.2.1.1)同工型I,II的活化剂进行了研究。 ,VII和XIV。一些衍生物显示出良好的活化和选择性分布。这项研究提供了一个有趣的机会来研究噻唑支架设计的CA激活剂(CAA),它可能作用于中枢神经系统,并靶向涉及记忆和学习障碍的病理学。