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.
MeSH terms
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Animals
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Asthma / drug therapy*
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Bronchodilator Agents / chemical synthesis*
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Bronchodilator Agents / pharmacology*
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Guinea Pigs
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology*
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In Vitro Techniques
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Male
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Phthalazines / chemical synthesis*
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Phthalazines / pharmacology*
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Rabbits
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
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Thromboxane A2 / metabolism*
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Thromboxane-A Synthase / antagonists & inhibitors*
Substances
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Bronchodilator Agents
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Imidazoles
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Phthalazines
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Thromboxane A2
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Thromboxane-A Synthase