Wenkang Guo , Manchun Chen , Changjie Zou , Weizhi Liu , Weidong Wang , Heyong Gao
{"title":"海藻酸寡糖衍生物的设计、合成和生物学评价。","authors":"Wenkang Guo , Manchun Chen , Changjie Zou , Weizhi Liu , Weidong Wang , Heyong Gao","doi":"10.1016/j.bmcl.2024.130039","DOIUrl":null,"url":null,"abstract":"<div><div>To discover new potential drug for acute kidney injury (AKI), a series of novel alginate oligosaccharide derivatives were synthesized and characterized by the spectroscopic analysis. By using the controlled experimental method, the target compounds were evaluated preliminarily for therapeutic activity in AKI. The results demonstrated that compounds <strong>2a</strong>, <strong>2b</strong>, <strong>2c</strong> and <strong>3b</strong> exhibited notable inhibitory activity against the expression of related proteins at 250 μg/ml in vitro. Furthermore, the in vivo activity of <strong>2a</strong> and <strong>2b</strong> was found to be comparable to that of the trisaccharide (AOSC).</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"116 ","pages":"Article 130039"},"PeriodicalIF":2.5000,"publicationDate":"2024-11-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, synthesis and biological evaluation of alginate oligosaccharide derivatives\",\"authors\":\"Wenkang Guo , Manchun Chen , Changjie Zou , Weizhi Liu , Weidong Wang , Heyong Gao\",\"doi\":\"10.1016/j.bmcl.2024.130039\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>To discover new potential drug for acute kidney injury (AKI), a series of novel alginate oligosaccharide derivatives were synthesized and characterized by the spectroscopic analysis. By using the controlled experimental method, the target compounds were evaluated preliminarily for therapeutic activity in AKI. The results demonstrated that compounds <strong>2a</strong>, <strong>2b</strong>, <strong>2c</strong> and <strong>3b</strong> exhibited notable inhibitory activity against the expression of related proteins at 250 μg/ml in vitro. Furthermore, the in vivo activity of <strong>2a</strong> and <strong>2b</strong> was found to be comparable to that of the trisaccharide (AOSC).</div></div>\",\"PeriodicalId\":256,\"journal\":{\"name\":\"Bioorganic & Medicinal Chemistry Letters\",\"volume\":\"116 \",\"pages\":\"Article 130039\"},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2024-11-23\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Bioorganic & Medicinal Chemistry Letters\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0960894X24004414\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0960894X24004414","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Design, synthesis and biological evaluation of alginate oligosaccharide derivatives
To discover new potential drug for acute kidney injury (AKI), a series of novel alginate oligosaccharide derivatives were synthesized and characterized by the spectroscopic analysis. By using the controlled experimental method, the target compounds were evaluated preliminarily for therapeutic activity in AKI. The results demonstrated that compounds 2a, 2b, 2c and 3b exhibited notable inhibitory activity against the expression of related proteins at 250 μg/ml in vitro. Furthermore, the in vivo activity of 2a and 2b was found to be comparable to that of the trisaccharide (AOSC).
期刊介绍:
Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.