Novel Antiasthematic Agents with Dual Activities of Thromboxane A2 Synthetase Inhibition and Bronchodilation. IV.2-[2-(1-Imidazolyl)ethyl]-4-(3-pyridyl-1(2H)-phthalazinones

Masahisa YAMAGUCHI; Takaki KOGA; Kenshi KAMEI; Michitaka AKIMA; Noriaki MARUYAMA; Toshio KUROKI; Masatomo HAMANA; Nobuhiro OHI

doi:10.1248/cpb.42.1850

Novel Antiasthematic Agents with Dual Activities of Thromboxane A₂ Synthetase Inhibition and Bronchodilation. IV.2-[2-(1-Imidazolyl)ethyl]-4-(3-pyridyl-1(2H)-phthalazinones

Masahisa YAMAGUCHI, Takaki KOGA, Kenshi KAMEI, Michitaka AKIMA, Noriaki MARUYAMA, Toshio KUROKI, Masatomo HAMANA, Nobuhiro OHI

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Keywords: phthalazinone, TXA₂ synthetase-inhibitory activity, bronchodiatory activity, antiasthmatic agent

JOURNAL FREE ACCESS

1994 Volume 42 Issue 9 Pages 1850-1853

DOI https://doi.org/10.1248/cpb.42.1850

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Abstract

Synthesis and pharmacological evaluation of several compounds related to 2-[2-(1-imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones are described. The phenyl moiety of the phthalazinone skeleton was found to play an important role in both thromboxane A₂ synthetase-inhibitory and bronchodilatory activities. Further, the 3-pyridyl group at the 4-position was shown to be necessary for in vivo thromboxane A₂ synthetase-inhibitory activity.

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