{"title":"具有芳基烷基和二芳基烷基取代的四氢吡啶亚基铵盐及其抗原虫活性","authors":"","doi":"10.1007/s00706-023-03142-8","DOIUrl":null,"url":null,"abstract":"<h3>Abstract</h3> <p>Tetrahydropyridin-4-ylidene salts with benzyl and dibenzyl substitution showed good antiprotozoal activity. This paper reports the synthesis of analogues with longer side chains. They were investigated for their antiprotozoal activities as well as for their cytotoxicity using microplate assays. The most active compounds showed activity against <em>Trypanosoma brucei rhodesiense</em> in concentrations < 0.06 µM. A series of compounds was active against <em>Plasmodium falciparum</em> NF54 in low nanomolar concentration and exhibited outstanding selectivity. The influence of substitution pattern and chain length on the antiprotozoal potencies were analyzed and structure–activity relationships were given. New compounds were characterized by FT-IR, HRMS, and NMR spectroscopy.</p> <span> <h3>Graphical abstract</h3> <p> <span> <span> <img alt=\"\" src=\"https://static-content.springer.com/image/MediaObjects/706_2023_3142_Figa_HTML.png\"/> </span> </span></p> </span>","PeriodicalId":19011,"journal":{"name":"Monatshefte für Chemie / Chemical Monthly","volume":"44 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2023-12-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Tetrahydropyridinylidene ammonium salts with arylalkyl and diarylalkyl substitution and their antiprotozoal activity\",\"authors\":\"\",\"doi\":\"10.1007/s00706-023-03142-8\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<h3>Abstract</h3> <p>Tetrahydropyridin-4-ylidene salts with benzyl and dibenzyl substitution showed good antiprotozoal activity. This paper reports the synthesis of analogues with longer side chains. They were investigated for their antiprotozoal activities as well as for their cytotoxicity using microplate assays. The most active compounds showed activity against <em>Trypanosoma brucei rhodesiense</em> in concentrations < 0.06 µM. A series of compounds was active against <em>Plasmodium falciparum</em> NF54 in low nanomolar concentration and exhibited outstanding selectivity. The influence of substitution pattern and chain length on the antiprotozoal potencies were analyzed and structure–activity relationships were given. New compounds were characterized by FT-IR, HRMS, and NMR spectroscopy.</p> <span> <h3>Graphical abstract</h3> <p> <span> <span> <img alt=\\\"\\\" src=\\\"https://static-content.springer.com/image/MediaObjects/706_2023_3142_Figa_HTML.png\\\"/> </span> </span></p> </span>\",\"PeriodicalId\":19011,\"journal\":{\"name\":\"Monatshefte für Chemie / Chemical Monthly\",\"volume\":\"44 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-12-27\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Monatshefte für Chemie / Chemical Monthly\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1007/s00706-023-03142-8\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Monatshefte für Chemie / Chemical Monthly","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1007/s00706-023-03142-8","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Tetrahydropyridinylidene ammonium salts with arylalkyl and diarylalkyl substitution and their antiprotozoal activity
Abstract
Tetrahydropyridin-4-ylidene salts with benzyl and dibenzyl substitution showed good antiprotozoal activity. This paper reports the synthesis of analogues with longer side chains. They were investigated for their antiprotozoal activities as well as for their cytotoxicity using microplate assays. The most active compounds showed activity against Trypanosoma brucei rhodesiense in concentrations < 0.06 µM. A series of compounds was active against Plasmodium falciparum NF54 in low nanomolar concentration and exhibited outstanding selectivity. The influence of substitution pattern and chain length on the antiprotozoal potencies were analyzed and structure–activity relationships were given. New compounds were characterized by FT-IR, HRMS, and NMR spectroscopy.
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