Dayanand N. Patagar , Raviraj Kusanur , Sheetal R. Batakurki , Maya Pai M , Vishnumurthy K. A , Swarna M. Patra , Aejaz A. Khan
{"title":"3-乙氧基羰基香豆素-8-丙酰胺的合成、抗氧化和抗糖尿病潜力评估","authors":"Dayanand N. Patagar , Raviraj Kusanur , Sheetal R. Batakurki , Maya Pai M , Vishnumurthy K. A , Swarna M. Patra , Aejaz A. Khan","doi":"10.1016/j.jics.2024.101465","DOIUrl":null,"url":null,"abstract":"<div><div>A series of 3- ethoxycarbonyl coumarin-8-propionamide analogues were designed, synthesized and <em>in vitro</em> antioxidant potential was screened by DPPH and ABTS assays and examined their anti-diabetic activity against α-amylase enzyme. The 3-fluoro-2-trifluoromethyl phenyl substituted coumarin-8-propionamide (<strong>8k</strong>) showed excellent scavenging potential (IC<sub>50</sub> - 43.1 μM) for both DPPH and ABTS free radicals compared with the standards trolox (IC<sub>50</sub> - 43.3 μM) and ascorbic acid (IC<sub>50</sub> - 42.1 μM). The compound dicyanophenyl substituted propionamide analogue (<strong>8m</strong>) displayed highest inhibition with IC<sub>50</sub> value of 5.1 μM against the α-amylase enzyme which is well comparable with Metformin (IC<sub>50</sub> 4.6 μM). The docking studies of the compounds with the receptor protein α-amylase (PDB ID 4x9y) shown lower binding energy when compared with Metformin.</div></div>","PeriodicalId":17276,"journal":{"name":"Journal of the Indian Chemical Society","volume":"101 12","pages":"Article 101465"},"PeriodicalIF":3.2000,"publicationDate":"2024-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis, evaluation of antioxidant and antidiabetic potential of 3-ethoxy carbonyl coumarin-8-propionamides\",\"authors\":\"Dayanand N. Patagar , Raviraj Kusanur , Sheetal R. Batakurki , Maya Pai M , Vishnumurthy K. A , Swarna M. Patra , Aejaz A. Khan\",\"doi\":\"10.1016/j.jics.2024.101465\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>A series of 3- ethoxycarbonyl coumarin-8-propionamide analogues were designed, synthesized and <em>in vitro</em> antioxidant potential was screened by DPPH and ABTS assays and examined their anti-diabetic activity against α-amylase enzyme. The 3-fluoro-2-trifluoromethyl phenyl substituted coumarin-8-propionamide (<strong>8k</strong>) showed excellent scavenging potential (IC<sub>50</sub> - 43.1 μM) for both DPPH and ABTS free radicals compared with the standards trolox (IC<sub>50</sub> - 43.3 μM) and ascorbic acid (IC<sub>50</sub> - 42.1 μM). The compound dicyanophenyl substituted propionamide analogue (<strong>8m</strong>) displayed highest inhibition with IC<sub>50</sub> value of 5.1 μM against the α-amylase enzyme which is well comparable with Metformin (IC<sub>50</sub> 4.6 μM). The docking studies of the compounds with the receptor protein α-amylase (PDB ID 4x9y) shown lower binding energy when compared with Metformin.</div></div>\",\"PeriodicalId\":17276,\"journal\":{\"name\":\"Journal of the Indian Chemical Society\",\"volume\":\"101 12\",\"pages\":\"Article 101465\"},\"PeriodicalIF\":3.2000,\"publicationDate\":\"2024-11-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of the Indian Chemical Society\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0019452224003455\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of the Indian Chemical Society","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0019452224003455","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Synthesis, evaluation of antioxidant and antidiabetic potential of 3-ethoxy carbonyl coumarin-8-propionamides
A series of 3- ethoxycarbonyl coumarin-8-propionamide analogues were designed, synthesized and in vitro antioxidant potential was screened by DPPH and ABTS assays and examined their anti-diabetic activity against α-amylase enzyme. The 3-fluoro-2-trifluoromethyl phenyl substituted coumarin-8-propionamide (8k) showed excellent scavenging potential (IC50 - 43.1 μM) for both DPPH and ABTS free radicals compared with the standards trolox (IC50 - 43.3 μM) and ascorbic acid (IC50 - 42.1 μM). The compound dicyanophenyl substituted propionamide analogue (8m) displayed highest inhibition with IC50 value of 5.1 μM against the α-amylase enzyme which is well comparable with Metformin (IC50 4.6 μM). The docking studies of the compounds with the receptor protein α-amylase (PDB ID 4x9y) shown lower binding energy when compared with Metformin.
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