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 , Irene Giorgi , Oreste Livi , Enrica Martinotti , Alma Martelli , 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 , Irene Giorgi , Oreste Livi , Enrica Martinotti , Alma Martelli , 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}
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.