Synthesis and antihyperglycemic evaluation of new 2,4-thiazolidinediones having biodynamic aryl sulfonylurea moieties
作者:Dhanaji V. Jawale、Umesh R. Pratap、Neha Rahuja、Arvind K. Srivastava、Ramrao A. Mane
DOI:10.1016/j.bmcl.2011.10.110
日期:2012.1
New 2,4-thiazolidinediones with aryl sulfonylurea moieties 8a–h have been synthesized by condensing various substituted sulfonamides and 5-(isocyanatomethyl) thiazolidino-2,4-dione 6. The isocyanomethyl thiazolidinedione was obtained by using the Curtius rearrangement, starting from known 2,4-dioxo-5-thiazolidineacetic acid 4. The newly synthesized compounds 8a–h have been evaluated for the antihyperglycemic
通过缩合各种取代的磺酰胺和5-(异氰酸根合甲基)噻唑烷二-2,4-二酮6合成了具有芳基磺酰脲部分8a - h的新2,4-噻唑烷二酮。异氰基甲基噻唑烷二酮是通过使用Curtius重排法从已知的2,4-二氧-5-噻唑烷乙酸4开始获得的。已经评估了新合成的化合物8a - h在正常大鼠模型中的抗降血糖活性,其中这些化合物8b,8c,8e和8f在负载蔗糖的大鼠模型中显示出显着的降血糖活性。