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 group...

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Bibliographic Details
Published in:	Chemical & pharmaceutical bulletin Vol. 43; no. 2; pp. 332 - 334
Main Authors:	YAMAGUCHI, Masahisa, MARUYAMA, Noriaki, KOGA, Takaki, KAMEI, Kenshi, AKIMA, Michitaka, KUROKI, Toshio, HAMANA, Masatomo, OHI, Nobuhiro
Format:	Journal Article
Language:	English
Published:	Tokyo The Pharmaceutical Society of Japan 1995 Maruzen
Subjects:	Administration, Oral Aminophylline - pharmacology Animals antiasthematic agent Benzofurans - pharmacology Biological and medical sciences bronchodilator Bronchodilator Agents - chemical synthesis Bronchodilator Agents - chemistry Bronchodilator Agents - pharmacology Fatty Acids, Monounsaturated - pharmacology Guinea Pigs Histamine Antagonists - chemical synthesis Histamine Antagonists - pharmacology In Vitro Techniques indazole derivative Indazoles - chemistry Indazoles - pharmacology Male Medical sciences Methacrylates - pharmacology Pentanoic Acids - pharmacology Pharmacology. Drug treatments Pyridines - pharmacology Rats Rats, Sprague-Dawley Respiratory system Structure-Activity Relationship Thromboxane-A Synthase - antagonists & inhibitors Thromboxane-A Synthase - blood Trachea - drug effects TXA2 synthetase inhibitor Intramolecular oxidoreductases Rat Enzyme Bronchodilator Rodentia Enzyme inhibitor Antiasthma agent In vitro Indazole derivatives Pyridine derivatives In vivo Vertebrata Isomerases Mammalia Guinea pig Thromboxane-A synthase Ex vivo Structure activity relation Animal Chemical synthesis
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Summary:	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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.43.332