Synthesis and Oral Hypoglycemic Activity of Some New Sulphonyl Linkage Thiazolidine-2,4-diones

International Journal of Pharmaceutical Sciences and Drug Research Pub Date : 2020-11-30 DOI:10.25004/ijpsdr.2020.120603

L. Kawale, V. Nade, R. Deshmukh, M. Dumbare

{"title":"Synthesis and Oral Hypoglycemic Activity of Some New Sulphonyl Linkage Thiazolidine-2,4-diones","authors":"L. Kawale, V. Nade, R. Deshmukh, M. Dumbare","doi":"10.25004/ijpsdr.2020.120603","DOIUrl":null,"url":null,"abstract":"Type 2 diabetes mellitus and its complications, decreases the quality of life in diabetic patients. Thiazolidine-2,4-diones are found to be better insulin sensitizing agents, acting on peroxisome proliferator activated receptor-γ (PPAR-γ) and decrease blood glucose level in diabetic patient. Therefore, in the present work, we synthesized 5-[4-(substituted) sulphonylbenzylidene]thiazolidine-2,4-diones and evaluated for their oral hypoglycemic activity. The synthesized compounds were further studied for their find out interactions with 2PRG protein with the help of docking score and also find out their predicated ED25 values. The results of synthesized compounds were showed significant decrease in blood glucose level as compared to positive control group. All synthesized compounds have shown good hydrogen bond interactions with 2PRG protein, docking score and predicted ED25 value as compared with reference drug, pioglitazone and rosiglitazone, respectively. Thus, sulphonyl linked thiazolidine-2,4-diones may be used as promising oral hypoglycemic agent.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"45 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2020-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Pharmaceutical Sciences and Drug Research","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.25004/ijpsdr.2020.120603","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}

引用次数: 0

Abstract

Type 2 diabetes mellitus and its complications, decreases the quality of life in diabetic patients. Thiazolidine-2,4-diones are found to be better insulin sensitizing agents, acting on peroxisome proliferator activated receptor-γ (PPAR-γ) and decrease blood glucose level in diabetic patient. Therefore, in the present work, we synthesized 5-[4-(substituted) sulphonylbenzylidene]thiazolidine-2,4-diones and evaluated for their oral hypoglycemic activity. The synthesized compounds were further studied for their find out interactions with 2PRG protein with the help of docking score and also find out their predicated ED25 values. The results of synthesized compounds were showed significant decrease in blood glucose level as compared to positive control group. All synthesized compounds have shown good hydrogen bond interactions with 2PRG protein, docking score and predicted ED25 value as compared with reference drug, pioglitazone and rosiglitazone, respectively. Thus, sulphonyl linked thiazolidine-2,4-diones may be used as promising oral hypoglycemic agent.

查看原文

微信好友朋友圈 QQ好友复制链接

本刊更多论文

新型磺酰基噻唑烷-2,4-二酮的合成及口服降糖活性研究

2型糖尿病及其并发症降低了糖尿病患者的生活质量。噻唑烷-2,4-二酮是较好的胰岛素增敏剂，可作用于过氧化物酶体增殖物激活受体-γ (PPAR-γ)，降低糖尿病患者的血糖水平。因此，本文合成了5-[4-(取代)磺基苄基]噻唑烷-2,4-二酮类化合物，并对其口服降糖活性进行了评价。通过对接评分进一步研究合成的化合物与2PRG蛋白的相互作用，并确定其预测的ED25值。结果表明，与阳性对照组相比，合成的化合物显著降低了血糖水平。与对照药物吡格列酮和罗格列酮相比，所有合成的化合物均与2PRG蛋白表现出良好的氢键相互作用，对接评分和ED25预测值均较好。因此，磺酰基连接噻唑烷-2,4-二酮可能是一种有前景的口服降糖药。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文去求助

来源期刊

International Journal of Pharmaceutical Sciences and Drug Research

自引率

0.00%

发文量