{"title":"介离子1-芳基-4-(苯基/对氯苯基)咪唑[2,1-b]噻唑-4酮的合成及其单胺氧化酶、琥珀酸脱氢酶抑制、抗惊厥和抗菌活性的研究","authors":"","doi":"10.33263/lianbs123.090","DOIUrl":null,"url":null,"abstract":"1-Aryl-2-mercapto-4-(phenyl/p-chlorophenyl)imidazoles (Ia-j) were condensed with monochloroacetic acid to give 1-aryl-4-(phenyl/p-chlorophenyl)imidazo-2-mercaptoacetic acid (IIa-j). These acids were subsequently cyclized with an acetic anhydride-pyridine mixture to give a new fused ring mesoionic 1-aryl-4-(phenyl/p-chlorophenyl)imidazo[2,1-b]thiazol-1-3-ones (IIIa-j). These compounds possess AID50 values ranging from 500 to 1000 mg kg-1, inhibit monoamineoxidase (32-68%), and succinate dehydrogenase (28-55%) in vitro at a concentration of 2×10-4 M, and provide 20-60% protection against pentylenetetrazole induced convulsions in mice.","PeriodicalId":18009,"journal":{"name":"Letters in Applied NanoBioScience","volume":"56 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2022-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis of Mesoionic 1-aryl-4-(phenyl/p-chlorophenyl)imidazo[2,1-b]thiazol-4-ones and Study of their Monoamine Oxidase, Succinate Dehydrogenase Inhibitory, Anti-convulsant, and Antibacterial Activity\",\"authors\":\"\",\"doi\":\"10.33263/lianbs123.090\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"1-Aryl-2-mercapto-4-(phenyl/p-chlorophenyl)imidazoles (Ia-j) were condensed with monochloroacetic acid to give 1-aryl-4-(phenyl/p-chlorophenyl)imidazo-2-mercaptoacetic acid (IIa-j). These acids were subsequently cyclized with an acetic anhydride-pyridine mixture to give a new fused ring mesoionic 1-aryl-4-(phenyl/p-chlorophenyl)imidazo[2,1-b]thiazol-1-3-ones (IIIa-j). These compounds possess AID50 values ranging from 500 to 1000 mg kg-1, inhibit monoamineoxidase (32-68%), and succinate dehydrogenase (28-55%) in vitro at a concentration of 2×10-4 M, and provide 20-60% protection against pentylenetetrazole induced convulsions in mice.\",\"PeriodicalId\":18009,\"journal\":{\"name\":\"Letters in Applied NanoBioScience\",\"volume\":\"56 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2022-05-22\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Letters in Applied NanoBioScience\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.33263/lianbs123.090\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Letters in Applied NanoBioScience","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.33263/lianbs123.090","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis of Mesoionic 1-aryl-4-(phenyl/p-chlorophenyl)imidazo[2,1-b]thiazol-4-ones and Study of their Monoamine Oxidase, Succinate Dehydrogenase Inhibitory, Anti-convulsant, and Antibacterial Activity
1-Aryl-2-mercapto-4-(phenyl/p-chlorophenyl)imidazoles (Ia-j) were condensed with monochloroacetic acid to give 1-aryl-4-(phenyl/p-chlorophenyl)imidazo-2-mercaptoacetic acid (IIa-j). These acids were subsequently cyclized with an acetic anhydride-pyridine mixture to give a new fused ring mesoionic 1-aryl-4-(phenyl/p-chlorophenyl)imidazo[2,1-b]thiazol-1-3-ones (IIIa-j). These compounds possess AID50 values ranging from 500 to 1000 mg kg-1, inhibit monoamineoxidase (32-68%), and succinate dehydrogenase (28-55%) in vitro at a concentration of 2×10-4 M, and provide 20-60% protection against pentylenetetrazole induced convulsions in mice.