Synthesis and Bioactivity of Propranolol Analogues with a Rigid Skeleton. I

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概要

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• The synthesis of two kinds of propranolol analogues, A and B, with a rigid skeleton was investigated. The compounds were designed to help identify the conformation involved in β-adrenergic receptor-propranolol interaction. The key intermediate, 2-hydroxy・2,3-dihydronaphtho[1,8-bc]pyran (5), was obtained starting from acenaphthenone (1). On sequential dehydration, hydroboration, and oxidation, 5 gave 2,3-dihydronaphtho[1,8-bc]pyran-3-one (8), which was converted to compound A. Compound 5 was also derived to 2-formyl-2,3-dihydronaphtho[1,8-bc]pyran (13) via the 2-vinyl compound (12). Condensation of nitromethane with 13 followed by reduction and alkylation produced the desired compound B. The β-blocking activities of A and B were examined.

• 社団法人日本薬学会の論文
• 1990-12-25

著者

• 竹村 庄司

  Faculty Of Pharmaceutical Sciences Kinki University

• 中野 彰子

  Faculties Of Pharmaceutical Sciences Kinki University

• 三木 康義

  Faculty of Pharmaceutical Sciences, Kinki University

• 野口 晃司

  Faculties Of Pharmaceutical Sciences Kinki University

• 八軒 浩子

  Faculties of Pharmaceutical Sciences, Kinki University

• 大田 真由美

  Faculties of Pharmaceutical Sciences, Kinki University

• 高橋 紘一

  Science and Technology, Kinki University

• 大田 真由美

  Faculties Of Pharmaceutical Sciences Kinki University

• 三木 康義

  Faculty Of Pharmaceutical Sciences Kinki University

• 八軒 浩子

  Faculties Of Pharmaceutical Sciences Kinki University

• 三木 康義

  近畿大学 薬学部

• 高橋 紘一

  Science And Technology Kinki University

• 竹村 庄司

  Faculty of Pharmaceutical Sciences, Kinki University

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