2007年1月
Analgesic agents without gastric damage: Design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors
BIOORGANIC & MEDICINAL CHEMISTRY
- ,
- ,
- ,
- ,
- ,
- ,
- ,
- ,
- ,
- 巻
- 15
- 号
- 2
- 開始ページ
- 1014
- 終了ページ
- 1021
- 記述言語
- 英語
- 掲載種別
- DOI
- 10.1016/j.bmc.2006.10.029
- 出版者・発行元
- PERGAMON-ELSEVIER SCIENCE LTD
In order to create novel analgesic agents without gastric disturbance, structurally simple cyclooxygenase-1 (COX-1) inhibitors with a benzenesulfonanilide skeleton were designed and synthesized. As a result, compounds 11f and 15a, which possess a p-amino group on the benzenesulfonyl moiety and p-chloro group on the anilino moiety, showed COX-1-selective inhibition. Moreover compound 11f, which is the most potent compound in this study showed more potent analgesic activity than that of aspirin at 30 mg/kg by po. The anti-inflammatory activity and gastric damage, however, were very weak or not detectably different from aspirin. Since the structure of our COX-1 inhibitors are very simple, they may be useful as lead compounds for superior COX-1 inhibitors as analgesic agents without gastric disturbance. (c) 2006 Published by Elsevier Ltd.
- リンク情報
- ID情報
-
- DOI : 10.1016/j.bmc.2006.10.029
- ISSN : 0968-0896
- Web of Science ID : WOS:000243315300039