2-苯基-1,3,4-噻二唑衍生物的合成与活性评价  

Synthesis and evaluation of 2-phenyl-1,3,4-thiadiazole derivatives

作　　者：朱锦锦 徐露玫 张丹 乔春华[1] ZHU Jin-jin;XU Lu-mei;ZHANG Dan;QIAO Chun-hua(School of Pharmaceutical Science,Soochow University,Suzhou 215123,China)

机构地区：[1]苏州大学药学院,江苏苏州215213

出　　处：《化学研究与应用》2018年第10期1668-1677,共10页Chemical Research and Application

摘　　要：合成18个2-苯基-1,3,4噻二唑系列化合物并评价其对吲哚胺2,3-双加氧酶1(Indoleamine 2,3-Dioxygenase1,IDO1)抑制活性。生物上建立酶活性检测体系,检测2-苯基-1,3,4噻二唑类化合物的IDO1抑制活性。结果表明对18个噻二唑类化合物进行酶活性检测,分析得到相关的构效关系,其中A16表现出较好的IDO1抑制活性。A series of 2-phenyl-1,3,4-thiadiazole derivatives were designed and evaluated as inhibitors of indoleamine 2,3-dioxygenase1(IDO1).According to the related literatures,18 chemical compounds were chemically synthesized in chemistry and an enzyme activity assay system was established in biology.The IDO1 inhibitory activity of 2-phenyl-1,3,4-thiadiazoles was also tested.Enzymatic activities of 18 thiadiazoles were detected and analyzed.The results showed that A16 showed better IDO1 inhibitory activity.

关 键 词：2-苯基-1 3 4噻二唑类 吲哚胺2 3-双加氧酶1 IDO1抑制剂 

分 类 号：O626.2[理学—有机化学]