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dibenzothiophene N,N-dimethyl-formamide 4-dibenzothiophene boronic acid Glyoxilic acid4-dibenzothienyl-2-(4,4-dimethyl-2-oxazolin-2-yl)phenylmethanol 4-styryldibenzothiophene dibenzo[b,d]-thiophene-4-ylmethanol 4-(2-formylbenzyl)dibenzothiophene 📜4-甲基二苯并噻吩置于正丁基锂体系中,用 四氢呋喃,正己烷 用作溶剂,化学反应 7.5H,以85%的收率获得二苯并噻吩-4-甲醛
参考文献:二芳基甲烷骨架的系统构效关系 (Sar) 探索和高效新型尿酸转运蛋白 1 (Urat1) 抑制剂的发现
标题:二芳基甲烷骨架的系统构效关系 (Sar) 探索和高效新型尿酸转运蛋白 1 (Urat1) 抑制剂的发现
摘要:为了系统地探索和更好地理解二芳基甲烷骨架在设计强效尿酸转运蛋白 1 (Urat1) 抑制剂时的构效关系 (Sar),设计并合成了 33 种化合物(1A-1X 和 1Ha-1Hi),并测定了它们的体外 Urat1 抑制活性 (Ic50).三轮系统的 Sar 探索导致发现了一种高效的新型 Urat1 抑制剂,1H,其效力分别比母体 Lesinurad 和苯溴马隆强 200 倍和 8 倍(ic50 = 0.035 μm 对人 Urat1 1 小时 Vs Lesinurad 和苯溴马隆分别为 7.18 μm 和 0.28 μm).化合物 1H 是迄今为止我们实验室发现的最有效的 Urat1 抑制剂,也可与目前正在临床试验中开发的最有效的抑制剂相媲美.
Doi:10.3390/molecules23020252
专利信息
专利号:US-2025189532-A1
优先权日:2022-03-04
标 题:1,6-diyne compound, its preparation method, and products obtained using 1,6-diyne compound as raw material and their applications
发明人:BAO HONGLI; YE CHANGQING; HUANG RUI; ZHU NENGBO
权利人:FUJIAN INST RES STR MATTER CAS
摘要:A 1,6-diynes compound, its preparation method, and products obtained from 1,6-diynes as raw material and their applications are provided. The compound represented by a general formula (I), and its tautomers, polymorphs, solvates, or salts thereof, n n n n n n n n n n The 1,6-diyne compounds provided have variable structures, are easy to be synthesized, and are suitable for industrial production; they can be used for the synthesis of a class of benzoisoindole dimer compounds and their derivatives, cell imaging, and detecting reactive oxygen species (such as sodium hypochlorite, hydrogen peroxide, ozone, etc.). The 3-arylbenzoisoindole compound provided can be used as an important compound and play an important role in pharmaceuticals or fluorescent materials.