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1990 Fiscal Year Final Research Report Summary

Researches of Synthesis and Antidepressive Evaluation of Azasteroid and Its Related Compounds

Research Project

Project/Area Number 01571152
Research Category

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

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

Principal Investigator

HIROTA Takashi  Okayama University Pharmaceutical Sciences Professor, 薬学部, 教授 (00033275)

Co-Investigator(Kenkyū-buntansha) OGASAWARA Sadanori  MECT Co. Ltd. Central Laboratory Subdirector, 研究所, 副所長
SASSAKI Kenji  Okayama University Pharmaceutical Sciences Research Associate, 薬学部, 助手 (20116461)
KATSU Takashi  Okayama University Pharmaceutical Scienses Research Associate, 薬学部, 助手 (40112156)
Project Period (FY) 1989 – 1990
KeywordsAntidepression / 11, 13, 15-Triazasteroid / Benzocycloheptapyrimidine / Antireserpine / B-Homoazasteroid / B, D-Dihomoazasteroid / 17-Oxide / 11, 13, 15, 17-Tetraazasteroid
Research Abstract

As one of the researches of synthesis of the compounds related to azasteroid and their evaluation of antidepressive activity using 11, 13, 15-triazasteroid (1) as a lead compound, B-homo-11, 13, 15-triazasteroids (2) bearing a alkyl group on D ring, B,D-dihomo-11, 13, 15-triaza-steroids (3) bearing a alkyl group on D ring, 6, 7-dihydro-5H-benzo [6, 7] cyclohepta [1, 2-d] pyrimidines (4) corresponding to D-secoazasteroid and bearing a alkylamino group on its 4-position, 11, 13, 15, 17-tetraazasteroids (5, n = 1) whose D ring was expanded to pyrimidine from imidazole, their B-homologue (5, n=2), and 17-oxides (6) of compound 5 were synthesized. Next, the evaluation of the antireserpine acivity of the above synthesized compounds and their precursors was performed as one of the first screening of the antidepressive activity. In compounds 2, only some tricyclic benzo [6, 7] cyclohepta [1, 2-d] pyrimidines which were precursors of corresponding tetracyclic azasteroid exhibited effective activity. In compounds 3, neither compounds 3 nor their precursors exhibited antireserpine activity. In compounds 4, only compounds, which have two carbon atoms between nitrogen atom attached to 4-position and oxygen atom at the terminal position of the side chain and also have branched side chain, exhibited effective one. In compounds, both 11, 13, 15, 17-tetraazasteroid without any substituent on its skeleton and ist B-homolgue exhibited effective activity. Their precursor, 4-amino-6, 7-dihydro -5H-benzo [6, 7] cyclohepta [1, 2-d] pyrimidine, also exhibited the similar one. In N-oxides (6), positive compounds could not be recognized.

  • Research Products

    (8 results)

All Other

All Publications (8 results)

  • [Publications] Takashi Hirota: "Synthesis and Antidepressive Evaluation of BーHomoー11,13,15ーtriazasteroids and Their Precursors" J.Heterocyclic Chem.27. 759-763 (1990)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Kenji Sasaki: "Synthesis of 4ーSubstituted 6,7ーDihydroー5Hーbenzo[6,7]cyclohepta[1,2ーd]ーpyrimidines and Their Inhibitory Activities on Platelet Aggregation and ReserpineーInduced Hypothermia" J.Heterocyclic Chem.27. 1771-1776 (1990)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Takashi Hirota: "Synthesis and Antidepressive Evaluation of 11,13,15,17ーTetraazasteroids and Their 17ーoxides" J.Heterocyclic Chem.

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Kenji Sasaki: "Synthesis of Novel B,DーDihomoー11,13,15ーtriazasteroidal Skeleton and Their Inhibitory Activity on Platelet Aggregation and Effect on ReserpineーIndcued Hypothermia" J.Heterocyclic Chem.

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Takashi Hirota: "Synthesis and Antidepressive Evaluation of B-Homo-11, 13, 15-triazasteroids and Their Precursors" J. Heterocyclic Chem.27. 759-763 (1990)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Kenji Sasaki: "Syntheses of 4-Substituted 6, 7-Dihydro-5H-benzo-[6, 7]cyclohepta[1, 2-d]pyrimidines and Their Inhibitory Activities on Platelet Aggregation and on Reserpine-Induced Hypothermia." J. Heterocyclic Chem.,. 27. 1771-1776 (1990)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Takashi Hirota: "Syntheses and Antidepressive Evaluation of 11, 13, 15, 17-Tetraazasteroids and Their 17-Oxides" J. Heterocylic Chem.

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Kenji Sasaki: "Synthesis of Novel B, D-Dihomo-11, 13, 15-triazasteroidal Skeleton and Their Inhibitory Activities on Platelet Aggregation and Effect on Reserpine-Induced Hypothermia." J. Heterocyclic Chem.

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

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Published: 1993-08-12  

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