Syntheses and Anti-inflammatory Activities of O-Acyloximes. II
スポンサーリンク
概要
- 論文の詳細を見る
Novel O-acyloximes having an acetyl group or N-protected amino acid as an O-acyl group were synthesized by reaction with acetyl chloride or by a mixed anhydride method. 4'-Morpholinoacetophenone oxime (oxime-2) was determined to be the (E) isomer by X-ray crystal structure analysis. The anti-inflammatory activities of the test compounds were assessed in terms of the inhibitory effect on increased vascular permeability induced by histamine, and several compounds were assessed together by means of the carrageenan-induced paw edema assay. In general, acetyl oximes and tert-butyloxycarbonylphenylalanyl oximes showed inhibitory action on increased vascular permeability. Particularly important for the appearance of anti-inflammatory activity was direct attachment of the acetyl group to the oxime. Of the two isoforms of cyclooxygenase (COX-1 and COX-2), COX-1 activity was inhibited by oxime-2 and 4'-piperidinoacetophenone oxime (oxime-3) with IC_<50> values of 50 and 130 μM, respectively, while COX-2 activity was not inhibited. The in vitro inhibitory effect of oxime-2 and oxime-3 on COX-1 activity decreased with O-acylation of the oximes.
- 公益社団法人日本薬学会の論文
- 1996-01-15
著者
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YAMAGATA Yuriko
Graduate School of Pharmaceutical Sciences, Kumamoto University
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Yamamoto Shuhei
Department Of Chemistry Graduate School Of Science Osaka City University
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Yamamoto K
Department Of Biochemistry Tokushima University School Of Medicine
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Yamamoto Kei
Department Of Chemical Engineering Faculty Of Engineering Tokyo Institute Of Technology
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Kataoka Hiromi
School Of Pharmaceutical Sciences Mukogawa Women 's University
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YAMAKI Masae
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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KATAOKA Hiromi
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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KATAGI Toyoshi
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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Yamagata Yuriko
Japan And Faculty Of Pharmaceutical Sciences Osaka University
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加多木 豊之
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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Yamamoto K
Faculty Of Pharmaceutical Sciences Josai University
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Yamaki M
Mukogawa Women's Univ. Nishinomiya Jpn
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Yamaki Masae
Faculty Of Pharmaceutical Sciences Mukogawa Women's University:pharmaceutical Research Center K
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Yamaki Masae
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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Konishi Yuriko
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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Katagi T
School Of Pharmaceutical Sciences Mukogawa Women 's University
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Yamamoto Shozo
Department Of Biochemistry Tokushima University School Of Medicine
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TAKATA Yuki
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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KITANO Sachiyo
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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INOI Takeshi
Faculty of Engineering, Kogakuin University
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Kitano S
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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Takata Y
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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Inoi T
Faculty Of Engineering Kogakuin University
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Yamamoto Kei
Department Of Anesthesiology Kansai Medical University
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Yamaki Masae
Faculty Of Pharmaceutical Science Mukogawa Women's University
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KITANO Sachiyo
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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TAKATA Yuki
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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