Studies on Agents with Vasodilator and β-Blocking Activities(5)Synthesis and Pharmacological Activity of the Optical Isomers of TZC-5665

• SEKI Toshimi

• KANADA Arihiro

• NAKAO Tomio

• SHIRAIWA Masahumi

• ASANO Hajime

• MIYAZAWA Katsuhiko

• ISHIMORI Tsutomu

• MINAMI Nobuyoshi

• SHIBATA Kenyu

• YASUDA Kikuo

書誌事項

タイトル別名

• Studies on Agents with Vasodilator and .BETA.-Blocking Activities. V. Synthesis and Pharmacological Activity of the Optical Isomers of TZC-5665.
• Studies on Agents with Vasodilator and

抄録

Synthesis of the four optical isomers of TZC-5665 (1), a candidate for the treatment of congestive heart failure, was achieved by the reaction of chiral diaminopyridazinone (2) with chiral glycidyl ether (3). The hypotensive and β-blocking activities of 1 and its optical isomers were examined when given intravenously into anesthetized rats. Furthermore these compounds were evaluated for inhibitory activity on cAMP phosphodiesterase III. Among the four optical isomers. R_A, S_B-one (1c) possessed the essential activities of TZC-5665 (1).

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 46 (1), 84-96, 1998

  公益社団法人 日本薬学会

キーワード

• chiral pyridazinone
• enantioselective synthesis
• asymmetric hydrogenation
• hypotensive activity
• β-blocking activity
• phosphodiesterase III-inhibitory activity

詳細情報

• CRID: 1390282679141186048
• NII論文ID: 110003616720
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.46.84
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 4395828
• PubMed: 9468640
• Web Site: http://id.ndl.go.jp/bib/4395828
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I4395828
• Web Site: http://www.jstage.jst.go.jp/article/cpb1958/46/1/46_1_84/_pdf
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可