{"title":"新型噻唑烷-4- 1取代噻唑衍生物的设计、硅研究、合成、表征和抗惊厥活性","authors":"","doi":"10.33263/briac134.366","DOIUrl":null,"url":null,"abstract":"A series of novel thiazolidine-4-one substituted thiazoles were prepared using multi-step synthesis and screened for their antiepileptic potency. The chemical nature of the prepared derivatives was confirmed using FT-IR, elemental analyses, Mass spectroscopy, and 1H-NMR. Molecular properties and antiepileptic potency of the novel thiazoles were predicted using in-silico models such as molinspiration online tool and molecular docking, respectively. In-vivo antiepileptic potency of the entire title compounds was determined using MES and scPTZ method. Additionally, the rotorod test was employed to determine the neurotoxicity of the synthesized derivatives. Entire title analogs displayed -varying degrees of antiepileptic and neurotoxicity potency. The pharmacological potency of tested compounds was compared with their chemical structures. 2-(4-Nitrophenyl)-3-(4-((4-phenylthiazol-2-ylimino)methyl)phenyl) thiazolidin-4-one (PTT6) was found to be the very active derivative of this series among thirteen tested derivatives. Thus, this analog may act as a lead molecule to find potent and safer antiepileptic drugs.","PeriodicalId":9026,"journal":{"name":"Biointerface Research in Applied Chemistry","volume":" ","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2022-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, In-Silico Studies, Synthesis, Characterization, and Anticonvulsant Activities of Novel Thiazolidin-4-One Substituted Thiazole Derivatives\",\"authors\":\"\",\"doi\":\"10.33263/briac134.366\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A series of novel thiazolidine-4-one substituted thiazoles were prepared using multi-step synthesis and screened for their antiepileptic potency. The chemical nature of the prepared derivatives was confirmed using FT-IR, elemental analyses, Mass spectroscopy, and 1H-NMR. Molecular properties and antiepileptic potency of the novel thiazoles were predicted using in-silico models such as molinspiration online tool and molecular docking, respectively. In-vivo antiepileptic potency of the entire title compounds was determined using MES and scPTZ method. Additionally, the rotorod test was employed to determine the neurotoxicity of the synthesized derivatives. Entire title analogs displayed -varying degrees of antiepileptic and neurotoxicity potency. The pharmacological potency of tested compounds was compared with their chemical structures. 2-(4-Nitrophenyl)-3-(4-((4-phenylthiazol-2-ylimino)methyl)phenyl) thiazolidin-4-one (PTT6) was found to be the very active derivative of this series among thirteen tested derivatives. Thus, this analog may act as a lead molecule to find potent and safer antiepileptic drugs.\",\"PeriodicalId\":9026,\"journal\":{\"name\":\"Biointerface Research in Applied Chemistry\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2022-10-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Biointerface Research in Applied Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.33263/briac134.366\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Biochemistry, Genetics and Molecular Biology\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Biointerface Research in Applied Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.33263/briac134.366","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Biochemistry, Genetics and Molecular Biology","Score":null,"Total":0}
Design, In-Silico Studies, Synthesis, Characterization, and Anticonvulsant Activities of Novel Thiazolidin-4-One Substituted Thiazole Derivatives
A series of novel thiazolidine-4-one substituted thiazoles were prepared using multi-step synthesis and screened for their antiepileptic potency. The chemical nature of the prepared derivatives was confirmed using FT-IR, elemental analyses, Mass spectroscopy, and 1H-NMR. Molecular properties and antiepileptic potency of the novel thiazoles were predicted using in-silico models such as molinspiration online tool and molecular docking, respectively. In-vivo antiepileptic potency of the entire title compounds was determined using MES and scPTZ method. Additionally, the rotorod test was employed to determine the neurotoxicity of the synthesized derivatives. Entire title analogs displayed -varying degrees of antiepileptic and neurotoxicity potency. The pharmacological potency of tested compounds was compared with their chemical structures. 2-(4-Nitrophenyl)-3-(4-((4-phenylthiazol-2-ylimino)methyl)phenyl) thiazolidin-4-one (PTT6) was found to be the very active derivative of this series among thirteen tested derivatives. Thus, this analog may act as a lead molecule to find potent and safer antiepileptic drugs.
期刊介绍:
Biointerface Research in Applied Chemistry is an international and interdisciplinary research journal that focuses on all aspects of nanoscience, bioscience and applied chemistry. Submissions are solicited in all topical areas, ranging from basic aspects of the science materials to practical applications of such materials. With 6 issues per year, the first one published on the 15th of February of 2011, Biointerface Research in Applied Chemistry is an open-access journal, making all research results freely available online. The aim is to publish original papers, short communications as well as review papers highlighting interdisciplinary research, the potential applications of the molecules and materials in the bio-field. Our aim is to encourage scientists to publish their experimental and theoretical results in as much detail as possible.