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1991 Fiscal Year Final Research Report Summary

Basic Studies on the Synthesis and Structure-Activity Relationship of Cardiovascular Drugs

Research Project

Project/Area Number 01430022
Research Category

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

Allocation TypeSingle-year Grants
Research Field Chemical pharmacy
Research InstitutionTohoku University

Principal Investigator

YAMANAKA Hiroshi  Tohoku Univ., Pharmaceutical Institute, Prof., 薬学部, 教授 (40004551)

Co-Investigator(Kenkyū-buntansha) HOSODA Hiroshi  Tohoku Univ., Pharmaceutical Institute, Prof., 薬学部, 助教授 (10004607)
SATOH Susumu  Tohoku Univ., Pharmaceutical Institute, Prof., 薬学部, 教授 (80004604)
NOZOE Shigeo  Tohoku Univ., Pharmaceutical Institute, Prof., 薬学部, 教授 (50013305)
FUKUMOTO Keiichiro  Tohoku Univ., Pharmaceutical Institute, Prof., 薬学部, 教授 (50004586)
KANEKO Chikara  Tohoku Univ., Pharmaceutical Institute, Prof., 薬学部, 教授 (40013833)
Project Period (FY) 1989 – 1991
KeywordsStructure-activity relationship / Hypotensive activity / 1, 2, 4-Triazine-3-carboxylic acids / 6-Alkykamino-3-pyridazinecarboxylic acids / Fusaric acid / Corey lactone / Digitoxigenin / ジギトキシン
Research Abstract

In order to find out new compounds affecting cardiovascular functions, the synthesis and evaluation of 1, 2, 4-triazine derivatives were mainly investigated. Although the moderate effect was observed on 5-substituted 1, 2, 4-triazine-3-carboxylic acids, 6-alkylamino-3-pyridazinecar-boxylic acids were found to be much more potent than 1, 2, 4-triazine derivatives.
Based on these results, structure-activity relationships of N-hetero-aromatic compounds as cardiovascular drugs was arranged satisfactory. In connection with the above research, some natural products, prostaglandin derivatives and synthetic intermediates of digitoxigenin were investigated, but in this fields, no compounds having hypotensive activity.

  • Research Products

    (21 results)

All Other

All Publications (21 results)

  • [Publications] Shoetsu Konno: "Synthesis of 6-Alkylamino-3-pyridhzinecarboxylic Acid Derivatives from Methyl 6-Chloro-3-pyridazinecarboxylate" Heterocycles. 34. 225-228 (1992)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Masayuki Sato: "Asymmetric de Mayo Reaction Using Chiral Spirocyclic Dioxinones" J.Heterocyclic Chem.28. 241-251 (1991)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Hideo Nemoto: "A Novel Approach to Optically Active trans-Benzo-perhydroindan" J.Chem.Soc.Chemical Communication. 705-706 (1991)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Yuichi Endo: "Favelines,Novel Tricyclic Benzocycloheptenes with Cytotoxic Activ7ties from Brazilian Plant,Cnidoscolus Phyllacmthus" Tetrahedron Lett.32. 3083-3086 (1991)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] M.Nomura: "Antihypertensive Effect of a New Dihydropyridine Calcium Entry Blocker in Concious Hypertensive and Normotensive Rats" Arzeim.-Forsch./Drug Res.39. 1542-1545 (1989)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Hiroshi Hosoda: "Enzyme Labelling in Steroid Enzyme Immunoassays.Comparison of the p-Nitrophenyl Ester and N-Succinimidyl Ester Methods" Chem.Pharm.Bull.39. 2373-2377 (1991)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 山中 宏,今野 昌悦: "医薬品の開発・第7巻 分子設計(首藤紘一編)複素環生理活性物質ーヘテロ原子の役割ー" 廣川書店, 29 (1990)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Mataichi Sagi: "A Facile Synthesis of Fusaric Acid from Thienyl-as-triazine Derivatives" Heterocycles. 29. 2249 (1989)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Shoetsu Konno: "Synthesis of 4, 5-Diarylthiazole Derivatives as Blood Platelet Aggregation Inhibitors" Yakugaku Zasshi. 110. 105 (1990)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Mataichi Sagi: "Intramolecular Reverse-Electron Demand Diels-Alder Reaction of 1, 2, 4-Triazine Derivatives" Heterocycles. 30. 1009 (1990)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Shoetsu Konno: "Synthesis of 6-Alkylamino-3-pyridazinecarboxylic Acid Derivatives from Methyl 6-Choloro-3-pyridazine-carboxylate" Heterocycles. 34. 225 (1992)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Masayuki Sato: "2-Monosubstituted 1.3-Dioxin-4-ones : Diastereo-facial Selectivity in Pericyclic Reactions and its Explanation" J. Chem. Soc., Perkin Trans.1. 1779 (1990)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Masayuki Sato: "Synthesis and Their Use in Enantiomerically Pure Corey Lactone Analogue Synthesis" Chem. Pharm. Bull.38. 336 (1990)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Hideo Nemoto: "A Highly Stereoselective Total Synthesis of (<plus-minus>)-Estrone and (<plus-minus>)-Adrenoste " J. Chem. Soc., Perkin Trans.1. 1639 (1991)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Hideo Nemoto: "A Novel Approach to Optically Active trans-Benzo-perhydroindan (2.3, 3a, 3b, 4, 5-Hexahydro-1H-benz e - indene)" J. Chem. Soc., Perkin Trans.705. (1991)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Shinji Fushiya: "Acromeric Acid C. A New Toxic Constituent of Clitocybe Acromelalga : An Efficient Isolation of Acromeric Acids" Tetrahedron Lett.31. 3083 (1990)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yuichi Endo: "Favelines, Novel Tricyclic Benzocycloheptens with Cytotoxic Activities from Brailian Plant, Cnidoscolus phyllacanthus" Tetrahedron Lett.32. 3083 (1991)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] M. Nomura: "Antihypertensive Effect of a New Dihydropyridine Calcium Entry Blocker in Consious Hypertensive and Normtensive Rats" Arzneim. -Forsch. /Drug Res.39. 1542 (1989)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Kiyoshi Chiba: "Effects of a Novel alpha1-Adrenoceptor antagonist, SGB-1534, on Adrenergically Induced Renal Vasocon-striction in Dogs" Eur. J. Pharmacol.176. 263 (1990)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Junichi Goto: "Determination of 5beta-Cholestanoic Acids in Human Urine by Gas Chromatography-Mass Spectrometry with Negative Ion Chemical Ionization Detection" J. Chromatography. 493. 245 (1989)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Hiroshi Hosoda: "Enzyme Labeling in Steroid Enzyme Immunoassays. Comparison of the p-Nitrophenyl Ester and N-Succinimidyl Ester Method" Chem. Pharm. Bull.39. 2373 (1991)

    • Description
      「研究成果報告書概要(欧文)」より

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Published: 1993-03-16  

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