Synthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitors
作者:İlhami Gulçin、Malahat Abbasova、Parham Taslimi、Zübeyir Huyut、Leyla Safarova、Afsun Sujayev、Vagif Farzaliyev、Şükrü Beydemir、Saleh H. Alwasel、Claudiu T. Supuran
DOI:10.1080/14756366.2017.1368019
日期:2017.1.1
synthesized by a reaction with hemiformals, which are prepared by the reaction of alcohols and formaldehyde. In this study, the inhibitory effects of these molecules were investigated against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) enzymes and carbonic anhydrase I, and II isoenzymes (hCA I and II). Both hCA isoenzymes were significantly inhibited by the recently synthesized molecules
含氮和硫原子的化合物可广泛用于工业,医学,生物技术和化学技术等各个领域。因此,开发了巯基苯并噻唑,巯基苯并恶唑和2-氨基噻唑的氨基甲基化和烷氧基甲基化反应。此外,巯基苯并恶唑和2-氨基噻唑的烷氧基甲基衍生物是通过与半缩醛反应合成的,半缩醛是通过醇与甲醛反应制得的。在这项研究中,研究了这些分子对乙酰胆碱酯酶(AChE),丁酰胆碱酯酶(BChE)酶和碳酸酐酶I和II同工酶(hCA I和II)的抑制作用。两种hCA同工酶均被最近合成的分子显着抑制,hCA I的Ki值在58-157 nM之间,hCA II为81-215 nM。此外,这些分子的BChE和AChE的Ki参数分别在23-88和18-78 nM范围内计算。