{"title":"利尿剂2,5-二取代-1,3,4-噻二唑的合成及评价研究","authors":"S. Jain, P. Mishra","doi":"10.9734/bpi/nicb/v2/12286d","DOIUrl":null,"url":null,"abstract":"Acetazolamide and Methazolamide are well known 1,3,4-thiadiazole derivatives exhibiting diuretic activity. Therefore, some newer 2,5-disubstituted-1,3,4-thiadiazoles were prepared and screened for diuretic activity. A few of the compounds namely IVa1, IVb2 and IVc2 showed good diuretic activity comparable with the standard drug acetazolamide. Properties of the synthesized compounds were calculated by using the software Osiris property explorer (peo). Morphilino analogs (IVa3 – IVd3) showed higher Druglikeness and Drug Score as compared to other analogs. Among morphilino analogs IVa3 is the most active compound therefore selected for bioisosteric approach for newer analog design using molopt software.","PeriodicalId":19155,"journal":{"name":"New Innovations in Chemistry and Biochemistry Vol. 2","volume":"8 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2021-08-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Study on Synthesis and Appraisal of Some 2,5-Disubstituted-1,3,4-Thiadiazoles as Diuretic Agents\",\"authors\":\"S. Jain, P. Mishra\",\"doi\":\"10.9734/bpi/nicb/v2/12286d\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Acetazolamide and Methazolamide are well known 1,3,4-thiadiazole derivatives exhibiting diuretic activity. Therefore, some newer 2,5-disubstituted-1,3,4-thiadiazoles were prepared and screened for diuretic activity. A few of the compounds namely IVa1, IVb2 and IVc2 showed good diuretic activity comparable with the standard drug acetazolamide. Properties of the synthesized compounds were calculated by using the software Osiris property explorer (peo). Morphilino analogs (IVa3 – IVd3) showed higher Druglikeness and Drug Score as compared to other analogs. Among morphilino analogs IVa3 is the most active compound therefore selected for bioisosteric approach for newer analog design using molopt software.\",\"PeriodicalId\":19155,\"journal\":{\"name\":\"New Innovations in Chemistry and Biochemistry Vol. 2\",\"volume\":\"8 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2021-08-26\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"New Innovations in Chemistry and Biochemistry Vol. 2\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.9734/bpi/nicb/v2/12286d\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"New Innovations in Chemistry and Biochemistry Vol. 2","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.9734/bpi/nicb/v2/12286d","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Study on Synthesis and Appraisal of Some 2,5-Disubstituted-1,3,4-Thiadiazoles as Diuretic Agents
Acetazolamide and Methazolamide are well known 1,3,4-thiadiazole derivatives exhibiting diuretic activity. Therefore, some newer 2,5-disubstituted-1,3,4-thiadiazoles were prepared and screened for diuretic activity. A few of the compounds namely IVa1, IVb2 and IVc2 showed good diuretic activity comparable with the standard drug acetazolamide. Properties of the synthesized compounds were calculated by using the software Osiris property explorer (peo). Morphilino analogs (IVa3 – IVd3) showed higher Druglikeness and Drug Score as compared to other analogs. Among morphilino analogs IVa3 is the most active compound therefore selected for bioisosteric approach for newer analog design using molopt software.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
