Amino Acids and Peptides. LIII. Synthesis and Biological Activities of Some Pseudo-Peptide Analogs of PKSI-527,a Plasma Kallikrein Selective Inhibitor : The Importance of the Peptide Backbone
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概要
- 論文の詳細を見る
Pseudo-peptide analogs of trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-4-aminophenyl acetic acid (PKSI-527,plasma kallikrein selective inhibitor), in which an amide bond (peptide bond) has been replaced by a CH_2-NH bond, i.e. trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-Ψ(CH_2-NH)-4-aminophenyl acetic acid (I), trans-4-aminomethylcyclohexanecarbonyl-Ψ(CH_2-NH)-L-phenylalanyl-4-aminophenyl acetic acid (II) and trans-4-aminomethylcyclohexanecarbonyl-D-phenylalanyl-Ψ(CH_2-NH)-4-aminophenyl acetic acid (III) were synthesized. These pseudo-peptide analogs did not exhibit any detectable inhibitory activity against plasma kallikrein (PK), plasmin (PL), urokinase (UK), thrombine (TH) or trypsin (TRY). These results indicate that both carbonyl groups in the PKSI-527 are important for the manifestation of potent inhibitory activity against plasma kallikrein.
- 公益社団法人日本薬学会の論文
- 1999-08-15
著者
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OKADA Yoshio
Faculty of Pharmaceutical Sciences, Kobe Gakuin University
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Yokoi T
Faculty Of Pharmaceutical Sciences Kobe Gakuin University
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Tsuda Yuko
Faculty Of Pharmaceutical Sciences Kobe Gakuin University:cooperative Research Center Of Life Scienc
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Tsuda Yuko
Faculty Of Pharmaceutical Science Kobe Gakuin University
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Okada Yoshio
Faculty Of Pharmaceutical Sciences Kobe Gakuin University
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Hijikata-Okunomiya Akiko
Faculty of Health Science, Kobe University School of Medicine
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Okamoto Shosuke
Kobe Research Projects on Thrombosis and Haemostasis
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Takahashi M
Research Center For Medicinal Plant Resources National Institute Of Biomedical Innovation
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FUKUMIZU Atsuko
Faculty of Pharmaceutical Sciences, Kobe Gakuin University
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TADA Mayako
Faculty of Pharmaceutical Sciences, Kobe Gakuin University
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WANAKA Keiko
Kobe Research Projects on Thrombosis and Haemostasis
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Hijikata‐okunomiya A
Faculty Of Health Science Kobe University School Of Medicine
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Hijikata-okunomiya Akiko
Faculty Of Health Science Kobe University School Of Medicine
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Okamoto Shosuke
Kobe Research Projects On Thrombosis And Haemostatis
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Wanaka Keiko
Kobe Research Projects On Thrombosis And Haemostatis
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Tada M
Faculty Of Pharmaceutical Sciences Kobe Gakuin University
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TADA Mayako
Kobe Research Projects on Thrombosis and Haemostasis
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TSUDA Yoko
Faculty of Pharmaceutical Sciences, Kobe Gakuin University
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Tsuda Y
Faculty Of Pharmaceutical Sciences And High Technology Research Center Kobe Gakuin University
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Fukumizu Atsuko
Faculty Of Pharmaceutical Sciences Kobe Gakuin University
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岡本 成羽
Molecular Chemistry Laboratory Takeda Chemical Industries Ltd.
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