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[6-芳基哒嗪酮类抗高血压药刚性结构衍生物的意外抗炎活性。I. 4,4a-二氢-5H-茚并[1,2-c]哒嗪-3-酮的合成与活性]

[Unexpected anti-inflammatory activity of rigid structure derivatives of 6-arylpyridazinone antihypertensives. I. Synthesis and activity of 4,4a-dihydro-5H-indeno[1,2c]pyridazin-3-ones].

作者信息

Cignarella G, Grella G, Loriga M, Curzu M M, Schiatti G

出版信息

Farmaco Sci. 1978 Nov;33(11):866-74.

PMID:744241
Abstract

The antihypertensive 5-methyl-6-p.cyanophenyl-4,5-dihydro-3(2H)-pyridazinone has been embodied in a rigid framework corresponding to a 4,4a-dihydro-5H-indeno[1,2-c]-3-pyridazinonic structure (II). The resulting 7-cyano derivative (IIc) was found to be devoid of antihypertensive activity. However this compound, as well as other members having structure (II), exhibited antiinflammatory properties.

摘要

抗高血压药物5-甲基-6-对氰基苯基-4,5-二氢-3(2H)-哒嗪酮已被构建在一个与4,4a-二氢-5H-茚并[1,2-c]-3-哒嗪酮结构(II)相对应的刚性骨架中。所得到的7-氰基衍生物(IIc)被发现没有抗高血压活性。然而,该化合物以及其他具有结构(II)的成员表现出抗炎特性。

相似文献

1
[Unexpected anti-inflammatory activity of rigid structure derivatives of 6-arylpyridazinone antihypertensives. I. Synthesis and activity of 4,4a-dihydro-5H-indeno[1,2c]pyridazin-3-ones].[6-芳基哒嗪酮类抗高血压药刚性结构衍生物的意外抗炎活性。I. 4,4a-二氢-5H-茚并[1,2-c]哒嗪-3-酮的合成与活性]
Farmaco Sci. 1978 Nov;33(11):866-74.
2
[Unexpected anti-inflammatory activity of rigid structures derived from 6-arylpyridazinone antihypertensive agents. II. Synthesis and activity of 5H-indeno(1,2-c)pyridazine and 5H-indeno(1,2-c)pyridazin-3-one].[源自6-芳基哒嗪酮类抗高血压药物的刚性结构的意外抗炎活性。II. 5H-茚并(1,2-c)哒嗪和5H-茚并(1,2-c)哒嗪-3-酮的合成与活性]
Farmaco Sci. 1979 Jan;34(1):72-80.
3
[Unexpected anti-inflammatory activity of rigid structures derived from antihypertensive 6-arylpyridazinones. III. Synthesis and activity of 7-fluoro- and 5-keto-5H-indeno(1,2-c)pyridozines].[源自抗高血压6-芳基哒嗪酮的刚性结构的意外抗炎活性。III. 7-氟-和5-酮-5H-茚并(1,2-c)哒嗪的合成与活性]
Farmaco Sci. 1982 Feb;37(2):133-44.
4
New congeners of antihypertensive and antithrombotic 7-amino or 7-acetyl-aminosubstituted-4,4a-dihydro-5H-indeno (1,2-c)pyridazin-3-ones.具有降压和抗血栓作用的7-氨基或7-乙酰氨基取代的4,4a-二氢-5H-茚并[1,2-c]哒嗪-3-酮的新类似物。
Farmaco Sci. 1988 Feb;43(2):169-79.
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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.5-芳基-6-甲基-4,5-二氢哒嗪-3(2H)酮及相关的5-芳基-6-甲基哒嗪-3(2H)酮的合成与药理研究
Farmaco Sci. 1988 Jun;43(6):539-49.
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Conformationally restricted congeners of hypotensive and platelet aggregation inhibitors: 6-aryl-5-methyl-4,5-dihydro-3(2H)-pyridazinones derived from 5H-indeno[1,2-c]pyridazine.降压和血小板聚集抑制剂的构象受限类似物:源自5H-茚并[1,2-c]哒嗪的6-芳基-5-甲基-4,5-二氢-3(2H)-哒嗪酮。
J Med Chem. 1986 Nov;29(11):2191-4. doi: 10.1021/jm00161a010.
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Some pyrrole substituted aryl pyridazinone and phthalazinone derivatives and their antihypertensive activities.一些吡咯取代的芳基哒嗪酮和酞嗪酮衍生物及其降压活性。
Eur J Med Chem. 2004 Dec;39(12):1089-95. doi: 10.1016/j.ejmech.2004.09.005.
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Synthesis and pharmacological evaluation of 4a-methyl-4,4a,5,6-tetrahydrothieno[2,3-h]cinnolin-3(2H)-ones.4a-甲基-4,4a,5,6-四氢噻吩并[2,3-h]噌啉-3(2H)-酮的合成与药理评价
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[3-Hydrazinepyridazine derivatives. III. Synthesis and anti-hypertensive activity of new 3-(2-acylhydrazine)-pyridazine-6-alkylamino substitutes].[3-肼基哒嗪衍生物。III。新型3-(2-酰肼基)-哒嗪-6-烷基氨基取代物的合成与抗高血压活性]
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Synthesis and biological evaluation of some new pyridazinone derivatives.合成及一些新的哒嗪酮衍生物的生物评价。
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Therapeutic Potential of Tricyclic Pyridazinone-Based Molecules: An Overview.基于三环哒嗪酮的分子的治疗潜力:综述。
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