Thomas E W, Nishizawa E E, Zimmermann D C, Williams D J
J Med Chem. 1985 Apr;28(4):442-6. doi: 10.1021/jm00382a009.
Routine screening of compounds for inhibition of collagen-induced platelet aggregation in vitro revealed 4,5-bis-(4-methoxyphenyl)-1,2,3-thiadiazole (2) was active and it represents the first example of a 1,2,3-thiadiazole with possible antithrombotic activity. In order to develop a structure-activity relationship for this heterocycle, a number of new 4(5)-mono- and -disubstituted 1,2,3-thiadiazoles were synthesized. These were tested in our screen and a number of additional active compounds were found. The most active compounds (2, 5a, 5b, and 6c) were those in which the heterocycle was substituted with benzene rings possessing para electron-donating groups.
对化合物进行常规体外筛选以检测其对胶原诱导的血小板聚集的抑制作用，结果显示4,5-双-(4-甲氧基苯基)-1,2,3-噻二唑（2）具有活性，它是具有潜在抗血栓活性的1,2,3-噻二唑的首个实例。为了建立该杂环的构效关系，合成了一系列新的4(5)-单取代和双取代的1,2,3-噻二唑。对这些化合物进行了我们的筛选测试，发现了一些其他活性化合物。活性最高的化合物（2、5a、5b和6c）是那些杂环被带有对位供电子基团的苯环取代的化合物。
