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Design of inhibitors for trypsin and trypsin-like enzymes carrying Schiff base copper chelate moiety.

Research Project

Project/Area Number 06672108
Research Category

Grant-in-Aid for General Scientific Research (C)

Allocation TypeSingle-year Grants
Research Field Chemical pharmacy
Research InstitutionHealth Sciences University of Hokkaido

Principal Investigator

TANIZAWA Kazutaka  Health Sciences Univ.of Hokkaido, Fac.of Pharm.Sci., Professor, 薬学部, 教授 (90001049)

Co-Investigator(Kenkyū-buntansha) TOYOTA Eiko  Health Sciences Univ.of Hokkaido, Fac.of Pharm.Sci., Instructor, 薬学部, 助手 (00103200)
Project Period (FY) 1994 – 1995
Project Status Completed (Fiscal Year 1995)
Budget Amount *help
¥2,100,000 (Direct Cost: ¥2,100,000)
Fiscal Year 1995: ¥700,000 (Direct Cost: ¥700,000)
Fiscal Year 1994: ¥1,400,000 (Direct Cost: ¥1,400,000)
KeywordsSchiff base / trypsin / trypsin-like enzymes / enzyme inhibitor / inverse substrates / amidine
Research Abstract

Studies on trypsin-specific compounds can aid the design of clinically useful compounds, since a variety of physiologically important enzymes have trypsin-like specificity. We are also interested in the formation of very stable chelates from alpha-amino acid, salicylaldehyde and copper ion. In this regards we studied an application of the chelate formation process to the preparation of a variety of trypsin inhibitors.
It was shown that salicylaldehyde derivatives carrying an amidinium group react spontaneously with alpha-amino acids to afford stable chelates. A wide variety of chelates compounds were successfully prepared. Inhibitory activity of these amidinium chelates toward trypsin was shown to be very strong. Some compounds synthesized in this work have been shown to be the strongest synthetic inhibitor ever known. It can be concluded that the series of compounds is informative for the elucidation of structure-activity relationship of trypsin inhibitors and for the design of clinically useful compounds. The results of the present work have been and will be published in three papers.

Report

(3 results)
  • 1995 Annual Research Report   Final Research Report Summary
  • 1994 Annual Research Report
  • Research Products

    (10 results)

All Other

All Publications (10 results)

  • [Publications] Kazutaka Tanizawa: "Derivation of diasteromeric Schiff base copper chelates from α-amino acid racemates and their chromatographic separation" Bioorganic Chem.22. 51-57 (1994)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1995 Final Research Report Summary
  • [Publications] Eiko Toyota: "Chromatographic separation of diasteromeric Schlff base copper (II) , nickel (II) , and zinc (II) chelates from α-amino acid racemates" Bioorganic Chem.24(No.1). (1996)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1995 Final Research Report Summary
  • [Publications] Eiko Toyota: "Appllcation of spontaneous Schiff base copper chelates formation process to the design α a trypsin inhlbitor" Chem. Phar. Bull.44(No.5). (1996)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1995 Final Research Report Summary
  • [Publications] Kazutaka Tanizawa: "Derivation of diastereomeric Schiff base copper chelates from alpha-amino acid racemates and their chromatographic separation" Bioorganic Chem.22. 51-57 (1994)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1995 Final Research Report Summary
  • [Publications] Eiko Toyota: "Chromatographic separation of diastereomeric Schiff base copper (II), nickel (II) and zinc (II) chelates from alpha-amino acid racemates" Bioorganic Chem.24 No.1. (1996)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1995 Final Research Report Summary
  • [Publications] Eiko Toyota: "Application of spontaneous Schiff base copper chelates formation process to the design of a trypsin inhibitor" Chem.Pharm.Bull.44 No.5. (1996)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1995 Final Research Report Summary
  • [Publications] Eiko Toyota: "Chromatographic separation of diasteromeric Schiff base copper (II), nickel (II), and zinc (II) chelates from α-amino acid racemates" Bioorganic Chem.24. (No.1) (1996)

    • Related Report
      1995 Annual Research Report
  • [Publications] Eiko Toyota: "Application of spontaneous Schiff base copper chelates formation process to the design of a trypsin inhibitor" Chem. Phar. Bull.44. (No.5) (1996)

    • Related Report
      1995 Annual Research Report
  • [Publications] Kazutaka Tanizawa: "Derivation of Diastereomeric Schiff Base Copper Chelates from α-Amino Acid Racemates and Their Chromatographic Separation" Bioorganic Chemistry. 22. 51-57 (1994)

    • Related Report
      1994 Annual Research Report
  • [Publications] Kazutaka Tanizawa: "Optically Active Compounds Derived from Salicylaldehyde and Pyridoxal" Bioorganic Chemistry. 21. 415-422 (1993)

    • Related Report
      1994 Annual Research Report

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Published: 1994-04-01   Modified: 2016-04-21  

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