{"title":"作为 AChE 和 BuChE 抑制剂和抗氧化剂的吡咯噻唑衍生物的设计、合成和评估","authors":"U. Acar Çevik, Tuğba Erçetin","doi":"10.17776/csj.1255826","DOIUrl":null,"url":null,"abstract":"Thiazole rings are one of the most frequently used heterocyclic moieties and are found in a wide variety of biologically active chemicals. In this research project, we report the synthesis and biological activities of some new thiazole derivatives (2a-2c) as potent anti-Alzheimer’s agents. These final compounds’ structures were characterized by spectral (1H NMR, 13C NMR, and MS spectra) analyses. The highest inhibitory activity against AChE was demonstrated by compound 2c (23.73 ± 0.018 %) with chloro substitution at the meta and para positions of the phenyl ring, while the highest inhibitory activity against BuChE was produced by compound 2a (28.87± 0.003 %) with cyano substitution at the f position of the phenyl ring. Ferrous ion-chelating and DPPH techniques were also used to assess the compounds' antioxidant properties. Compound 2a showed antioxidant effect according to the DPPH method with an IC50 value of 27.18 ± 0.009 µM.","PeriodicalId":10906,"journal":{"name":"Cumhuriyet Science Journal","volume":"52 s33","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2023-12-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Synthesis and Evaluation of Pyrrol-thiazole Derivatives as AChE and BuChE Inhibitory and Antioxidant Activities\",\"authors\":\"U. Acar Çevik, Tuğba Erçetin\",\"doi\":\"10.17776/csj.1255826\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Thiazole rings are one of the most frequently used heterocyclic moieties and are found in a wide variety of biologically active chemicals. In this research project, we report the synthesis and biological activities of some new thiazole derivatives (2a-2c) as potent anti-Alzheimer’s agents. These final compounds’ structures were characterized by spectral (1H NMR, 13C NMR, and MS spectra) analyses. The highest inhibitory activity against AChE was demonstrated by compound 2c (23.73 ± 0.018 %) with chloro substitution at the meta and para positions of the phenyl ring, while the highest inhibitory activity against BuChE was produced by compound 2a (28.87± 0.003 %) with cyano substitution at the f position of the phenyl ring. Ferrous ion-chelating and DPPH techniques were also used to assess the compounds' antioxidant properties. Compound 2a showed antioxidant effect according to the DPPH method with an IC50 value of 27.18 ± 0.009 µM.\",\"PeriodicalId\":10906,\"journal\":{\"name\":\"Cumhuriyet Science Journal\",\"volume\":\"52 s33\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-12-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Cumhuriyet Science Journal\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.17776/csj.1255826\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Cumhuriyet Science Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.17776/csj.1255826","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Design, Synthesis and Evaluation of Pyrrol-thiazole Derivatives as AChE and BuChE Inhibitory and Antioxidant Activities
Thiazole rings are one of the most frequently used heterocyclic moieties and are found in a wide variety of biologically active chemicals. In this research project, we report the synthesis and biological activities of some new thiazole derivatives (2a-2c) as potent anti-Alzheimer’s agents. These final compounds’ structures were characterized by spectral (1H NMR, 13C NMR, and MS spectra) analyses. The highest inhibitory activity against AChE was demonstrated by compound 2c (23.73 ± 0.018 %) with chloro substitution at the meta and para positions of the phenyl ring, while the highest inhibitory activity against BuChE was produced by compound 2a (28.87± 0.003 %) with cyano substitution at the f position of the phenyl ring. Ferrous ion-chelating and DPPH techniques were also used to assess the compounds' antioxidant properties. Compound 2a showed antioxidant effect according to the DPPH method with an IC50 value of 27.18 ± 0.009 µM.