Synthesis of ortho-Functionalized 4-Aminomethylpyridazines as Substrate-Like Semicarbazide-Sensitive Amine Oxidase Inhibitors
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- Haider Norbert
- Department of Drug and Natural Product Synthesis, Faculty of Life Sciences, University of Vienna
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- Hochholdinger Iris
- Department of Drug and Natural Product Synthesis, Faculty of Life Sciences, University of Vienna
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- Mátyus Péter
- Department of Organic Chemistry, Semmelweis University
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- Wobus Andrea
- Department of Drug and Natural Product Synthesis, Faculty of Life Sciences, University of Vienna
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A series of 4-aminomethylpyridazines and -pyridazin-3(2H)-ones (“diaza-benzylamines”), bearing alkylamino side chains in ortho position relative to the CH2NH2 unit, was synthesized by catalytic hydrogenation of the corresponding nitriles in strongly acidic medium. N-Benzyl protecting groups either at the pyridazinone ring nitrogen or at an exocyclic nitrogen were selectively removed hydrogenolytically or by treatment with a Lewis acid. The new compounds were tested in vitro for semicarbazide-sensitive amine oxidase (SSAO) inhibitory activity and 4-(aminomethyl)-N,N′-diethylpyridazine-3,5-diamine (22) was found to be the most active representative.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 58 (7), 964-970, 2010
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204173481984
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- NII論文ID
- 130000299795
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 10737782
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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- 抄録ライセンスフラグ
- 使用不可