Rifhat Sultana, Obaid-ur-Rahman Abid, Saira Bibi, Mohsin Ali, Syed Maeen Badshah, Shoaib Khan, Zaheed Ahmed
{"title":"脂肪酯类isatin衍生物的合成、酶抑制及对接研究","authors":"Rifhat Sultana, Obaid-ur-Rahman Abid, Saira Bibi, Mohsin Ali, Syed Maeen Badshah, Shoaib Khan, Zaheed Ahmed","doi":"10.1007/s13738-025-03250-8","DOIUrl":null,"url":null,"abstract":"<div><p>A series of imine derivatives of isatin 4(a–e), 5(a–e), 6(a–b) were synthesized using aliphatic hydrazides and substituted isatins. Synthesized products were analyzed by spectroanalytical techniques and evaluated for urease and <i>α</i>-glucosidase inhibition activities. Compounds 3a, 3b, 4b, 5a, 5b, 5c and 6a with an IC<sub>50</sub> values 50.40 ± 0.21, 46.19 ± 0.21, 46.03 ± 1.22, 43.33 ± 0.62, 50.67 ± 0.13, 45.78 ± 3.53, 50.34 ± 1.92 [µM] respectively exhibited excellent urease inhibition results compared to the standard [24.14 µM]. However with respect to α-glucosidase inhibition activity, the compounds 3b, 4a, 5a, 5b, and 5c with IC<sub>50</sub> values 133.08 ± 0.24, 162.15 ± 0.32, 128.56 ± 2.42, 136.70 ± 3.22 and 145.33 ± 0.32 [µM] respectively showed good inhibition. Results were also supported by docking studies.</p></div>","PeriodicalId":676,"journal":{"name":"Journal of the Iranian Chemical Society","volume":"22 8","pages":"1629 - 1636"},"PeriodicalIF":2.3000,"publicationDate":"2025-07-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis, enzyme inhibition and docking studies of isatin derivatives from aliphatic esters\",\"authors\":\"Rifhat Sultana, Obaid-ur-Rahman Abid, Saira Bibi, Mohsin Ali, Syed Maeen Badshah, Shoaib Khan, Zaheed Ahmed\",\"doi\":\"10.1007/s13738-025-03250-8\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>A series of imine derivatives of isatin 4(a–e), 5(a–e), 6(a–b) were synthesized using aliphatic hydrazides and substituted isatins. Synthesized products were analyzed by spectroanalytical techniques and evaluated for urease and <i>α</i>-glucosidase inhibition activities. Compounds 3a, 3b, 4b, 5a, 5b, 5c and 6a with an IC<sub>50</sub> values 50.40 ± 0.21, 46.19 ± 0.21, 46.03 ± 1.22, 43.33 ± 0.62, 50.67 ± 0.13, 45.78 ± 3.53, 50.34 ± 1.92 [µM] respectively exhibited excellent urease inhibition results compared to the standard [24.14 µM]. However with respect to α-glucosidase inhibition activity, the compounds 3b, 4a, 5a, 5b, and 5c with IC<sub>50</sub> values 133.08 ± 0.24, 162.15 ± 0.32, 128.56 ± 2.42, 136.70 ± 3.22 and 145.33 ± 0.32 [µM] respectively showed good inhibition. Results were also supported by docking studies.</p></div>\",\"PeriodicalId\":676,\"journal\":{\"name\":\"Journal of the Iranian Chemical Society\",\"volume\":\"22 8\",\"pages\":\"1629 - 1636\"},\"PeriodicalIF\":2.3000,\"publicationDate\":\"2025-07-27\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of the Iranian Chemical Society\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s13738-025-03250-8\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of the Iranian Chemical Society","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1007/s13738-025-03250-8","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Synthesis, enzyme inhibition and docking studies of isatin derivatives from aliphatic esters
A series of imine derivatives of isatin 4(a–e), 5(a–e), 6(a–b) were synthesized using aliphatic hydrazides and substituted isatins. Synthesized products were analyzed by spectroanalytical techniques and evaluated for urease and α-glucosidase inhibition activities. Compounds 3a, 3b, 4b, 5a, 5b, 5c and 6a with an IC50 values 50.40 ± 0.21, 46.19 ± 0.21, 46.03 ± 1.22, 43.33 ± 0.62, 50.67 ± 0.13, 45.78 ± 3.53, 50.34 ± 1.92 [µM] respectively exhibited excellent urease inhibition results compared to the standard [24.14 µM]. However with respect to α-glucosidase inhibition activity, the compounds 3b, 4a, 5a, 5b, and 5c with IC50 values 133.08 ± 0.24, 162.15 ± 0.32, 128.56 ± 2.42, 136.70 ± 3.22 and 145.33 ± 0.32 [µM] respectively showed good inhibition. Results were also supported by docking studies.
期刊介绍:
JICS is an international journal covering general fields of chemistry. JICS welcomes high quality original papers in English dealing with experimental, theoretical and applied research related to all branches of chemistry. These include the fields of analytical, inorganic, organic and physical chemistry as well as the chemical biology area. Review articles discussing specific areas of chemistry of current chemical or biological importance are also published. JICS ensures visibility of your research results to a worldwide audience in science. You are kindly invited to submit your manuscript to the Editor-in-Chief or Regional Editor. All contributions in the form of original papers or short communications will be peer reviewed and published free of charge after acceptance.