Xianfeng Huang, Yuanyuan Liu, Cheng Zhang, Guoqiang Song
{"title":"新型阿魏酸衍生物的合成、降糖及醛糖还原酶抑制活性","authors":"Xianfeng Huang, Yuanyuan Liu, Cheng Zhang, Guoqiang Song","doi":"10.7439/IJPC.V7I1.3798","DOIUrl":null,"url":null,"abstract":"A novel class of ferulic acid derivatives with urea groups were synthesized and evaluated for hypoglycemic and aldose reductase inhibition activities. Several compounds showed comparable in vivo hypoglycemic agents to the commercial drug glibenclamide. Furthermore, of the tested compounds, 7a and 7 b displayed the most potent aldose reductase inhibitory activity in vitro , with an IC 50 of 0.55 and 3.88 M, respectively. Docking simulation was performed to insert compound 7a and 12a into the crystal structure of aldose reductase at active site to determine the probable binding model.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"43 1","pages":"01-10"},"PeriodicalIF":0.0000,"publicationDate":"2017-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis, hypoglycemic and aldose reductase inhibition activity of novel ferulic acid derivatives\",\"authors\":\"Xianfeng Huang, Yuanyuan Liu, Cheng Zhang, Guoqiang Song\",\"doi\":\"10.7439/IJPC.V7I1.3798\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A novel class of ferulic acid derivatives with urea groups were synthesized and evaluated for hypoglycemic and aldose reductase inhibition activities. Several compounds showed comparable in vivo hypoglycemic agents to the commercial drug glibenclamide. Furthermore, of the tested compounds, 7a and 7 b displayed the most potent aldose reductase inhibitory activity in vitro , with an IC 50 of 0.55 and 3.88 M, respectively. Docking simulation was performed to insert compound 7a and 12a into the crystal structure of aldose reductase at active site to determine the probable binding model.\",\"PeriodicalId\":14317,\"journal\":{\"name\":\"International Journal of Pharmaceutical Chemistry\",\"volume\":\"43 1\",\"pages\":\"01-10\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2017-01-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International Journal of Pharmaceutical Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.7439/IJPC.V7I1.3798\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Pharmaceutical Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.7439/IJPC.V7I1.3798","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis, hypoglycemic and aldose reductase inhibition activity of novel ferulic acid derivatives
A novel class of ferulic acid derivatives with urea groups were synthesized and evaluated for hypoglycemic and aldose reductase inhibition activities. Several compounds showed comparable in vivo hypoglycemic agents to the commercial drug glibenclamide. Furthermore, of the tested compounds, 7a and 7 b displayed the most potent aldose reductase inhibitory activity in vitro , with an IC 50 of 0.55 and 3.88 M, respectively. Docking simulation was performed to insert compound 7a and 12a into the crystal structure of aldose reductase at active site to determine the probable binding model.