1,4-和2,4-取代-1,2,3-三唑作为潜在的钾通道活化剂。7

Vincenzo Calderone , Irene Giorgi , Oreste Livi , Enrica Martinotti , Alma Martelli , Antonio Nardi
{"title":"1,4-和2,4-取代-1,2,3-三唑作为潜在的钾通道活化剂。7","authors":"Vincenzo Calderone ,&nbsp;Irene Giorgi ,&nbsp;Oreste Livi ,&nbsp;Enrica Martinotti ,&nbsp;Alma Martelli ,&nbsp;Antonio Nardi","doi":"10.1016/j.farmac.2005.03.004","DOIUrl":null,"url":null,"abstract":"<div><p>New 1,4- and 2,4-substituted 1,2,3-triazole derivatives were synthesized and tested as potential BK<sub>Ca</sub><span><span> channel openers, as a part of a research program, which hypothesizes a pharmacophoric structure containing the 1,2,3-triazole ring. The structure–activity relationships were studied introducing some structural changes concerning molecular geometry and the presence of a hydrogen bond<span> donor as a primary amino group and a phenolic or alcoholic hydroxy function. The compounds were prepared by nucleophilic substitution on the 1,2,3-triazole ring and by 1,3-dipolar cycloaddition of azides to selected </span></span>alkynes and to phenylacetone. The new compounds tested on rat aortic rings did not exhibit any significant vasorelaxing activity.</span></p></div>","PeriodicalId":77128,"journal":{"name":"Farmaco (Societa chimica italiana : 1989)","volume":"60 5","pages":"Pages 367-375"},"PeriodicalIF":0.0000,"publicationDate":"2005-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.farmac.2005.03.004","citationCount":"11","resultStr":"{\"title\":\"1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII\",\"authors\":\"Vincenzo Calderone ,&nbsp;Irene Giorgi ,&nbsp;Oreste Livi ,&nbsp;Enrica Martinotti ,&nbsp;Alma Martelli ,&nbsp;Antonio Nardi\",\"doi\":\"10.1016/j.farmac.2005.03.004\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>New 1,4- and 2,4-substituted 1,2,3-triazole derivatives were synthesized and tested as potential BK<sub>Ca</sub><span><span> channel openers, as a part of a research program, which hypothesizes a pharmacophoric structure containing the 1,2,3-triazole ring. The structure–activity relationships were studied introducing some structural changes concerning molecular geometry and the presence of a hydrogen bond<span> donor as a primary amino group and a phenolic or alcoholic hydroxy function. The compounds were prepared by nucleophilic substitution on the 1,2,3-triazole ring and by 1,3-dipolar cycloaddition of azides to selected </span></span>alkynes and to phenylacetone. The new compounds tested on rat aortic rings did not exhibit any significant vasorelaxing activity.</span></p></div>\",\"PeriodicalId\":77128,\"journal\":{\"name\":\"Farmaco (Societa chimica italiana : 1989)\",\"volume\":\"60 5\",\"pages\":\"Pages 367-375\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2005-05-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/j.farmac.2005.03.004\",\"citationCount\":\"11\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Farmaco (Societa chimica italiana : 1989)\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0014827X05000650\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Farmaco (Societa chimica italiana : 1989)","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0014827X05000650","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 11

摘要

合成了新的1,4-和2,4-取代的1,2,3-三唑衍生物,并作为潜在的BKCa通道打开剂进行了测试,作为研究计划的一部分,该研究假设含有1,2,3-三唑环的药效结构。研究了结构与活性的关系,引入了分子几何结构的变化以及作为一级氨基的氢键供体和酚或醇羟基的存在。这些化合物是通过在1,2,3-三唑环上亲核取代和将叠氮化物与选定的炔和苯丙酮进行1,3-偶极环加成制备的。在大鼠主动脉环上测试的新化合物没有表现出任何显著的血管松弛活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII

New 1,4- and 2,4-substituted 1,2,3-triazole derivatives were synthesized and tested as potential BKCa channel openers, as a part of a research program, which hypothesizes a pharmacophoric structure containing the 1,2,3-triazole ring. The structure–activity relationships were studied introducing some structural changes concerning molecular geometry and the presence of a hydrogen bond donor as a primary amino group and a phenolic or alcoholic hydroxy function. The compounds were prepared by nucleophilic substitution on the 1,2,3-triazole ring and by 1,3-dipolar cycloaddition of azides to selected alkynes and to phenylacetone. The new compounds tested on rat aortic rings did not exhibit any significant vasorelaxing activity.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信