Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. IV. 2-[2-(1-Imidazolyl)ethyl]-4-(3-pyridyl)-1(2H)-phthalazinones.
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.
Fuji-gotemba Research Laboratories, Chugai Pharmaceutical Company, Ltd., Shizuoka, Japan.
M
M
Yamaguchi
T
T
Koga
K
K
Kamei
M
M
Akima
N
N
Maruyama
T
T
Kuroki
M
M
Hamana
N
N
Ohi
D000818:Animals; D001249:Asthma / Q000188:drug therapy*; D001993:Bronchodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D006168:Guinea Pigs; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D010793:Phthalazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013928:Thromboxane A2 / Q000378:metabolism*; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors*
D001993:Bronchodilator Agents; D007093:Imidazoles; D010793:Phthalazines; D013928:Thromboxane A2; D013930:Thromboxane-A Synthase