Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. VI. Indazole derivatives.
Synthesis and pharmacological evaluation of novel indazole derivatives are described. These compounds were found to exhibit both thromboxane A2 (TXA2) synthetase-inhibitory and bronchodilatory activities. This observation supports the idea that the partial structure of the 3-pyridyl and phenyl groups with a methylene insertion is an important component for well-balanced activities.
Yamaguchi
M
M
Fuji-gotemba Research Laboratories, Chugai Pharmaceutical Company, Ltd. Shizuoka, Japan.
Maruyama
N
N
Koga
T
T
Kamei
K
K
Akima
M
M
Kuroki
T
T
Hamana
M
M
Ohi
N
N
D000284:Administration, Oral; D000628:Aminophylline / Q000494:pharmacology; D000818:Animals; D001572:Benzofurans / Q000494:pharmacology; D001993:Bronchodilator Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005229:Fatty Acids, Monounsaturated / Q000494:pharmacology; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D066298:In Vitro Techniques; D007191:Indazoles / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D008689:Methacrylates / Q000494:pharmacology; D010421:Pentanoic Acids / Q000494:pharmacology; D011725:Pyridines / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D013930:Thromboxane-A Synthase / Q000037:antagonists & inhibitors* / Q000097:blood; D014132:Trachea / Q000187:drug effects
D001572:Benzofurans; D001993:Bronchodilator Agents; D005229:Fatty Acids, Monounsaturated; D006633:Histamine Antagonists; D007191:Indazoles; D008689:Methacrylates; D010421:Pentanoic Acids; D011725:Pyridines; D000628:Aminophylline; D013930:Thromboxane-A Synthase; C045446:isbogrel; C039936:furegrelate; C034364:ozagrel; C060219:ridogrel