{"title":"具有抗痉挛活性γ-(4-取代哌嗪-1-基)-α-苯基丙醇不对称酯衍生物的合成","authors":"P. O. Osadebe, P. Akah, C. O. Okafor, L. Natova","doi":"10.1211/146080800128735539","DOIUrl":null,"url":null,"abstract":"Six new ester derivatives of γ-(4-substituted piperazinyl)-α-phenyl propanol were prepared by esterification of the γ-piperazinyl propanols. \n \n \n \nThe derivatives were methyl, ethyl, phenyl and benzyl esters, and they were obtained in good yields using a solid-liquid phase transfer catalysed esterification method. The nitrogen content of the new derivatives was also determined. Studies using isolated guineapig ileum showed that the derivatives possessed varying degrees of antispasmodic activity. \n \n \n \nOf the compounds evaluated, the ethyl ester of γ-(4-benzyl piperazin-1-yl)-α-phenyl propanol showed the greatest antispasmodic activity.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2000-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis of Some Unsymmetrical Ester Derivatives of γ-(4-Substituted piperazin-1-yl)-α-phenyl propanols with Antispasmodic Activity\",\"authors\":\"P. O. Osadebe, P. Akah, C. O. Okafor, L. Natova\",\"doi\":\"10.1211/146080800128735539\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Six new ester derivatives of γ-(4-substituted piperazinyl)-α-phenyl propanol were prepared by esterification of the γ-piperazinyl propanols. \\n \\n \\n \\nThe derivatives were methyl, ethyl, phenyl and benzyl esters, and they were obtained in good yields using a solid-liquid phase transfer catalysed esterification method. The nitrogen content of the new derivatives was also determined. Studies using isolated guineapig ileum showed that the derivatives possessed varying degrees of antispasmodic activity. \\n \\n \\n \\nOf the compounds evaluated, the ethyl ester of γ-(4-benzyl piperazin-1-yl)-α-phenyl propanol showed the greatest antispasmodic activity.\",\"PeriodicalId\":19946,\"journal\":{\"name\":\"Pharmacy and Pharmacology Communications\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2000-10-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmacy and Pharmacology Communications\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1211/146080800128735539\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmacy and Pharmacology Communications","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1211/146080800128735539","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis of Some Unsymmetrical Ester Derivatives of γ-(4-Substituted piperazin-1-yl)-α-phenyl propanols with Antispasmodic Activity
Six new ester derivatives of γ-(4-substituted piperazinyl)-α-phenyl propanol were prepared by esterification of the γ-piperazinyl propanols.
The derivatives were methyl, ethyl, phenyl and benzyl esters, and they were obtained in good yields using a solid-liquid phase transfer catalysed esterification method. The nitrogen content of the new derivatives was also determined. Studies using isolated guineapig ileum showed that the derivatives possessed varying degrees of antispasmodic activity.
Of the compounds evaluated, the ethyl ester of γ-(4-benzyl piperazin-1-yl)-α-phenyl propanol showed the greatest antispasmodic activity.