Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. III. 4-[2-(5-ethyl-2-thienyl)]-2'-[2-(1-imidazolyl)ethyl]-1(2H)- phthalazinones.
Synthesis and pharmacological evaluation of novel 4-[2-(5-ethyl-2-thienyl)]-2-[2-(1-imidazolyl)ethyl]-1(2H)-phthalazinone s 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.
Fuji-gotemba Research Laboratories, Chugai Pharmaceutical Company, Ltd., Shizuoka, Japan.
M
M
Yamaguchi
T
T
Koga
K
K
Kamei
M
M
Akima
T
T
Kuroki
M
M
Hamana
N
N
Ohi
D000818:Animals; D001249:Asthma / Q000188:drug therapy; D001792:Blood Platelets / Q000187:drug effects; D016084:Bronchoconstriction / Q000187:drug effects*; D001993:Bronchodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D006224:Cricetinae; D015195:Drug Design; D004341:Drug Evaluation; D006168:Guinea Pigs; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D066298:In Vitro Techniques; D008297:Male; D010793:Phthalazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors*; D014132:Trachea / Q000187:drug effects
D001993:Bronchodilator Agents; D007093:Imidazoles; D010793:Phthalazines; D013930:Thromboxane-A Synthase