{"title":"噻唑烷二酮作为 PPAR-γ 激动剂的吉祥支架:对抗胰岛素抵抗性糖尿病的可能机制","authors":"Sourav Basak , Anjali Murmu , Balaji Wamanrao Matore , Partha Pratim Roy , Jagadish Singh","doi":"10.1016/j.ejmcr.2024.100160","DOIUrl":null,"url":null,"abstract":"<div><p>Thiazolidinedione (TZD) plays a crucial role in activating PPAR-γ receptor, which helps to inhibit insulin-resistant diabetes mellitus through binding with DNA by forming a complex with retinoid receptors. TZD derivatives are the sulphur and nitrogen containing heterocyclic compounds that have a massive impact in synthetic chemistry for their plethora of pharmacological activities. TZD helps to improve insulin resistance and lowering the blood glucose level through oxidation of carbohydrate in case of type II diabetes mellitus. TZD scaffold is a pentacyclic sulphur-containing compound with two carbonyl groups and an alpha hydrogen offering a huge possibility in structural modification of this biologically active molecule, here N-3 & C-5 positions are the most versatile site for structural modification in TZD nucleus. In this review, we focus on a brief description of its antidiabetic activity with its mechanism of action, structure activity relationship and various synthetic approach of the main pharmacophore TZD and hope it will help to develop idea about this moiety for future researchers.</p></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"11 ","pages":"Article 100160"},"PeriodicalIF":0.0000,"publicationDate":"2024-04-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2772417424000323/pdfft?md5=68c3388befc11daa705625582c3f7820&pid=1-s2.0-S2772417424000323-main.pdf","citationCount":"0","resultStr":"{\"title\":\"Thiazolidinedione an auspicious scaffold as PPAR-γ agonist: its possible mechanism to Manoeuvre against insulin resistant diabetes mellitus\",\"authors\":\"Sourav Basak , Anjali Murmu , Balaji Wamanrao Matore , Partha Pratim Roy , Jagadish Singh\",\"doi\":\"10.1016/j.ejmcr.2024.100160\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Thiazolidinedione (TZD) plays a crucial role in activating PPAR-γ receptor, which helps to inhibit insulin-resistant diabetes mellitus through binding with DNA by forming a complex with retinoid receptors. TZD derivatives are the sulphur and nitrogen containing heterocyclic compounds that have a massive impact in synthetic chemistry for their plethora of pharmacological activities. TZD helps to improve insulin resistance and lowering the blood glucose level through oxidation of carbohydrate in case of type II diabetes mellitus. TZD scaffold is a pentacyclic sulphur-containing compound with two carbonyl groups and an alpha hydrogen offering a huge possibility in structural modification of this biologically active molecule, here N-3 & C-5 positions are the most versatile site for structural modification in TZD nucleus. In this review, we focus on a brief description of its antidiabetic activity with its mechanism of action, structure activity relationship and various synthetic approach of the main pharmacophore TZD and hope it will help to develop idea about this moiety for future researchers.</p></div>\",\"PeriodicalId\":12015,\"journal\":{\"name\":\"European Journal of Medicinal Chemistry Reports\",\"volume\":\"11 \",\"pages\":\"Article 100160\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-04-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.sciencedirect.com/science/article/pii/S2772417424000323/pdfft?md5=68c3388befc11daa705625582c3f7820&pid=1-s2.0-S2772417424000323-main.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Medicinal Chemistry Reports\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2772417424000323\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry Reports","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2772417424000323","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Thiazolidinedione an auspicious scaffold as PPAR-γ agonist: its possible mechanism to Manoeuvre against insulin resistant diabetes mellitus
Thiazolidinedione (TZD) plays a crucial role in activating PPAR-γ receptor, which helps to inhibit insulin-resistant diabetes mellitus through binding with DNA by forming a complex with retinoid receptors. TZD derivatives are the sulphur and nitrogen containing heterocyclic compounds that have a massive impact in synthetic chemistry for their plethora of pharmacological activities. TZD helps to improve insulin resistance and lowering the blood glucose level through oxidation of carbohydrate in case of type II diabetes mellitus. TZD scaffold is a pentacyclic sulphur-containing compound with two carbonyl groups and an alpha hydrogen offering a huge possibility in structural modification of this biologically active molecule, here N-3 & C-5 positions are the most versatile site for structural modification in TZD nucleus. In this review, we focus on a brief description of its antidiabetic activity with its mechanism of action, structure activity relationship and various synthetic approach of the main pharmacophore TZD and hope it will help to develop idea about this moiety for future researchers.