3, 5-Diphenyl-1H-pyrazole衍生品。1-(2-羟乙基)-3,5-二苯基- 1h -吡唑及其4-溴衍生物的酯类和n -取代氨基甲酸酯类,具有抑制、抗心律失常、镇痛等活性。

F. Bondavalli, O. Bruno, A. Ranise, P. Schenone, P. Addonizio, V. de Novellis, A. Loffreda, E. Marmo
{"title":"3, 5-Diphenyl-1H-pyrazole衍生品。1-(2-羟乙基)-3,5-二苯基- 1h -吡唑及其4-溴衍生物的酯类和n -取代氨基甲酸酯类,具有抑制、抗心律失常、镇痛等活性。","authors":"F. Bondavalli, O. Bruno, A. Ranise, P. Schenone, P. Addonizio, V. de Novellis, A. Loffreda, E. Marmo","doi":"10.1002/CHIN.198912181","DOIUrl":null,"url":null,"abstract":"The synthesis of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole (II) and its 4-bromo derivative (III) starting from chalcone epoxide, as well as of a series of esters and N-substituted carbamates derived from (II) and (III), is described. Some of these compounds showed remarkable depressant, antiarrhythmic and analgesic activities in mice and rats. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardic and antiinflammatory activities in rats, infiltration anesthesia and hypoglycemic activity in mice, as well as a weak platelet antiaggregating activity in vitro.","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"81 1","pages":"725-43"},"PeriodicalIF":0.0000,"publicationDate":"1988-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities.\",\"authors\":\"F. Bondavalli, O. Bruno, A. Ranise, P. Schenone, P. Addonizio, V. de Novellis, A. Loffreda, E. Marmo\",\"doi\":\"10.1002/CHIN.198912181\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The synthesis of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole (II) and its 4-bromo derivative (III) starting from chalcone epoxide, as well as of a series of esters and N-substituted carbamates derived from (II) and (III), is described. Some of these compounds showed remarkable depressant, antiarrhythmic and analgesic activities in mice and rats. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardic and antiinflammatory activities in rats, infiltration anesthesia and hypoglycemic activity in mice, as well as a weak platelet antiaggregating activity in vitro.\",\"PeriodicalId\":13279,\"journal\":{\"name\":\"Il Farmaco; edizione scientifica\",\"volume\":\"81 1\",\"pages\":\"725-43\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1988-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Il Farmaco; edizione scientifica\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1002/CHIN.198912181\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Il Farmaco; edizione scientifica","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1002/CHIN.198912181","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

摘要

描述了以环氧查尔酮为起始原料合成1-(2-羟乙基)-3,5-二苯基- 1h -吡唑(II)及其4-溴衍生物(III),以及由(II)和(III)衍生的一系列酯和n -取代氨基甲酸酯。其中部分化合物对小鼠和大鼠具有显著的抑制、抗心律失常和镇痛作用。此外,上述化合物通常在大鼠中表现出中度的降压、心动过缓和抗炎活性,在小鼠中表现出浸润麻醉和降糖活性,在体外表现出弱的血小板抗聚集活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities.
The synthesis of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole (II) and its 4-bromo derivative (III) starting from chalcone epoxide, as well as of a series of esters and N-substituted carbamates derived from (II) and (III), is described. Some of these compounds showed remarkable depressant, antiarrhythmic and analgesic activities in mice and rats. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardic and antiinflammatory activities in rats, infiltration anesthesia and hypoglycemic activity in mice, as well as a weak platelet antiaggregating activity in vitro.
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
期刊最新文献
Synthesis, binding affinities for alpha-adrenoceptor and eudismic analysis of chiral benzodioxane derivatives and their chiral opened analogues. Prolyl derivatives of enalapril as potential angiotensin converting enzyme inhibitors. Synthesis, structure and activity of a few open models related to classic H2-antagonists. Benzodioxanes and quinazolines: probes for characterizing alpha-adrenoreceptors. Isolation and structure determination of the main related substances of teicoplanin, a glycopeptide antibiotic.
×
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
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 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 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1