Synthesis and Biological Activities of Optical Isomers of 2-(4-Diphenylmethyl-1-piperazinyl)ethyl Methyl 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate (Manidipine) Dihydrochloride

1 Citations
  • KAJINO M.
    Central Research Division, Takeda Chemical Industries, Ltd.,
  • WADA Yoshikazu
    Central Research Division, Takeda Chemical Industries, Ltd.,
  • NAGAI Yasuo
    Central Research Division, Takeda Chemical Industries, Ltd.,
  • NAGAOKA Akinobu
    Central Research Division, Takeda Chemical Industries, Ltd.,
  • MEGURO Kanji
    Central Research Division, Takeda Chemical Industries, Ltd.,

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Description

Enantiomeric (+)- and (-)-manidipine (1) dihydrochlorides were synthesized by the esterification of the optically active monocarboxylic acids (-)-6 and (+)-6,respectively. The absolute configurations, (S)-(+)-1 and (R)-(-)-1,were unambiguously determined by X-ray crystallographic analysis of (+)-7 derived from (-)-6. The (S)-(+)-1 was about 30 and 80 times as potent as the (R)-(-)-isomer in antihypertensive activity in spontaneously hypertensive rats (SHR), and in the radioligand binding assay using [^3H]nitrendipine, respectively.

Journal

  • Chem. Pharm. Bull.

    Chem. Pharm. Bull. 37 2225-2228, 1989

    The Pharmaceutical Society of Japan

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Details 詳細情報について

  • CRID
    1570854177484898048
  • NII Article ID
    110003627962
  • NII Book ID
    AA00602100
  • ISSN
    00092363
  • Text Lang
    en
  • Data Source
    • CiNii Articles

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