5-芳基-6-甲基-4,5-二氢吡啶嗪-3(2H)及相关5-芳基-6-甲基-吡啶嗪-3(2H)的合成及药理研究。

Il Farmaco; edizione scientifica Pub Date : 1988-06-01
G A Pinna, M M Curzu, D Barlocco, G Cignarella, E Cavalletti, M Germini, K Berger
{"title":"5-芳基-6-甲基-4,5-二氢吡啶嗪-3(2H)及相关5-芳基-6-甲基-吡啶嗪-3(2H)的合成及药理研究。","authors":"G A Pinna,&nbsp;M M Curzu,&nbsp;D Barlocco,&nbsp;G Cignarella,&nbsp;E Cavalletti,&nbsp;M Germini,&nbsp;K Berger","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>New 5-aryl-6-methyl-4,5-dihydropyridazin-3(2H)ones (III) and related 5-aryl-6-methyl-pyridazin-3(2H)ones (IV) were synthesized in order to evaluate their pharmacological profile in comparison with that of the known class of antihypertensive and platelet aggregation inhibitors 5-methyl-6-aryl-4,5-dihydropyridazin 3(2H)ones (I). Though none of the tested derivatives was found to possess the antihypertensive potency of the reference compounds, some of them displayed significant antithrombotic and antiulcer properties. In particular, 5(p. acetylaminophenyl)-6-methyl-pyridazin-3-one (IV c) was found highly effective (ED50 = 1.2 mg/kg) in inhibiting indomethacin-induced ulcers.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 6","pages":"539-49"},"PeriodicalIF":0.0000,"publicationDate":"1988-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and pharmacological study of 5-aryl-6-methyl-4,5-dihydro-pyridazin-3(2H)ones and related 5-aryl-6-methyl-pyridazin-3(2H)ones.\",\"authors\":\"G A Pinna,&nbsp;M M Curzu,&nbsp;D Barlocco,&nbsp;G Cignarella,&nbsp;E Cavalletti,&nbsp;M Germini,&nbsp;K Berger\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>New 5-aryl-6-methyl-4,5-dihydropyridazin-3(2H)ones (III) and related 5-aryl-6-methyl-pyridazin-3(2H)ones (IV) were synthesized in order to evaluate their pharmacological profile in comparison with that of the known class of antihypertensive and platelet aggregation inhibitors 5-methyl-6-aryl-4,5-dihydropyridazin 3(2H)ones (I). Though none of the tested derivatives was found to possess the antihypertensive potency of the reference compounds, some of them displayed significant antithrombotic and antiulcer properties. In particular, 5(p. acetylaminophenyl)-6-methyl-pyridazin-3-one (IV c) was found highly effective (ED50 = 1.2 mg/kg) in inhibiting indomethacin-induced ulcers.</p>\",\"PeriodicalId\":13279,\"journal\":{\"name\":\"Il Farmaco; edizione scientifica\",\"volume\":\"43 6\",\"pages\":\"539-49\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1988-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Il Farmaco; edizione scientifica\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"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":"","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

我们合成了新的5-芳基-6-甲基-4,5-二氢吡啶嗪-3(2H)化合物(III)和相关的5-芳基-6-甲基-4,5-二氢吡啶嗪-3(2H)化合物(IV),以便与已知的一类抗高血压和血小板聚集抑制剂(5-甲基-6-芳基-4,5-二氢吡啶嗪3(2H)化合物(I)进行药理学分析。其中一些具有显著的抗血栓和抗溃疡特性。特别是5(p。乙酰氨基苯基(acetylaminphenyl)-6-methyl-pyridazin-3-one (IV c)对吲哚美辛诱导的溃疡有良好的抑制作用(ED50 = 1.2 mg/kg)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Synthesis and pharmacological study of 5-aryl-6-methyl-4,5-dihydro-pyridazin-3(2H)ones and related 5-aryl-6-methyl-pyridazin-3(2H)ones.

New 5-aryl-6-methyl-4,5-dihydropyridazin-3(2H)ones (III) and related 5-aryl-6-methyl-pyridazin-3(2H)ones (IV) were synthesized in order to evaluate their pharmacological profile in comparison with that of the known class of antihypertensive and platelet aggregation inhibitors 5-methyl-6-aryl-4,5-dihydropyridazin 3(2H)ones (I). Though none of the tested derivatives was found to possess the antihypertensive potency of the reference compounds, some of them displayed significant antithrombotic and antiulcer properties. In particular, 5(p. acetylaminophenyl)-6-methyl-pyridazin-3-one (IV c) was found highly effective (ED50 = 1.2 mg/kg) in inhibiting indomethacin-induced ulcers.

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