{"title":"苯妥英类衍生物的合成及其中枢神经系统活性。","authors":"Rahul Chauhan, Shwetank Verma, Alankar Shrivasatava","doi":"10.2174/1871524922666220429122141","DOIUrl":null,"url":null,"abstract":"BACKGROUND\nThe derivatives of Phenytoin conjugated with various anilines were synthesized. The synthesized derivatives were evaluated for different physicochemical parameters along with Log P values using different software programs to discover its ability to cross the blood brain barrier. The pharmacological activities such as antianxiety, skeletal muscle relaxant and anticonvulsant were evaluated by using different models.\n\n\nOBJECTIVE\nThe new Phenytoin derivatives were synthesized and evaluated for different properties to predict its CNS activity. The drugs synthesized by chloroacetylation and then different aniline were added into it. The compounds were evaluated for their different CNS activity by using different methods.\n\n\nMETHOD\nThe compounds were synthesized by firstly chloroacetylating the phenytoin and then different substituted aniline were added into it. The compounds were evaluated for antianxiety activity, Muscle relaxant activity and anticonvulsant activity by using different models.\n\n\nRESULT\nThe number of derivatives of Phenytoin was synthesized and various physicochemical parameters were optimized which reveal that the compound containing chloro group such as C2 and C5 exhibited significant potential when compared with the standard drug Diazepam.\n\n\nCONCLUSION\nIt was portrayed that the synthesis, computational studies and evaluation of anticonvulsant, antianxiety and skeletal muscle relaxant activity of new Phenytoin derivatives were carried out. The compounds were productively synthesized and portrayed by molecular docking studies. The compounds also exhibit mild to moderate similarity with respect to standard drug. The synthesized drugs have the potential to be optimized further to engender new scaffolds to treat various CNS disorders.","PeriodicalId":9799,"journal":{"name":"Central nervous system agents in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and CNS Activity of Phenytoin derivatives.\",\"authors\":\"Rahul Chauhan, Shwetank Verma, Alankar Shrivasatava\",\"doi\":\"10.2174/1871524922666220429122141\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"BACKGROUND\\nThe derivatives of Phenytoin conjugated with various anilines were synthesized. The synthesized derivatives were evaluated for different physicochemical parameters along with Log P values using different software programs to discover its ability to cross the blood brain barrier. The pharmacological activities such as antianxiety, skeletal muscle relaxant and anticonvulsant were evaluated by using different models.\\n\\n\\nOBJECTIVE\\nThe new Phenytoin derivatives were synthesized and evaluated for different properties to predict its CNS activity. The drugs synthesized by chloroacetylation and then different aniline were added into it. The compounds were evaluated for their different CNS activity by using different methods.\\n\\n\\nMETHOD\\nThe compounds were synthesized by firstly chloroacetylating the phenytoin and then different substituted aniline were added into it. The compounds were evaluated for antianxiety activity, Muscle relaxant activity and anticonvulsant activity by using different models.\\n\\n\\nRESULT\\nThe number of derivatives of Phenytoin was synthesized and various physicochemical parameters were optimized which reveal that the compound containing chloro group such as C2 and C5 exhibited significant potential when compared with the standard drug Diazepam.\\n\\n\\nCONCLUSION\\nIt was portrayed that the synthesis, computational studies and evaluation of anticonvulsant, antianxiety and skeletal muscle relaxant activity of new Phenytoin derivatives were carried out. The compounds were productively synthesized and portrayed by molecular docking studies. The compounds also exhibit mild to moderate similarity with respect to standard drug. The synthesized drugs have the potential to be optimized further to engender new scaffolds to treat various CNS disorders.\",\"PeriodicalId\":9799,\"journal\":{\"name\":\"Central nervous system agents in medicinal chemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2022-04-29\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Central nervous system agents in medicinal chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1871524922666220429122141\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Psychology\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Central nervous system agents in medicinal chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1871524922666220429122141","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Psychology","Score":null,"Total":0}
Synthesis and CNS Activity of Phenytoin derivatives.
BACKGROUND
The derivatives of Phenytoin conjugated with various anilines were synthesized. The synthesized derivatives were evaluated for different physicochemical parameters along with Log P values using different software programs to discover its ability to cross the blood brain barrier. The pharmacological activities such as antianxiety, skeletal muscle relaxant and anticonvulsant were evaluated by using different models.
OBJECTIVE
The new Phenytoin derivatives were synthesized and evaluated for different properties to predict its CNS activity. The drugs synthesized by chloroacetylation and then different aniline were added into it. The compounds were evaluated for their different CNS activity by using different methods.
METHOD
The compounds were synthesized by firstly chloroacetylating the phenytoin and then different substituted aniline were added into it. The compounds were evaluated for antianxiety activity, Muscle relaxant activity and anticonvulsant activity by using different models.
RESULT
The number of derivatives of Phenytoin was synthesized and various physicochemical parameters were optimized which reveal that the compound containing chloro group such as C2 and C5 exhibited significant potential when compared with the standard drug Diazepam.
CONCLUSION
It was portrayed that the synthesis, computational studies and evaluation of anticonvulsant, antianxiety and skeletal muscle relaxant activity of new Phenytoin derivatives were carried out. The compounds were productively synthesized and portrayed by molecular docking studies. The compounds also exhibit mild to moderate similarity with respect to standard drug. The synthesized drugs have the potential to be optimized further to engender new scaffolds to treat various CNS disorders.
期刊介绍:
Central Nervous System Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new central nervous system agents. Containing a series of timely in-depth reviews written by leaders in the field covering a range of current topics, Central Nervous System Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in the field.