Synthesis and Biological Evaluation of Derivatives of 2-{2-Fluoro-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic Acid: Nonsteroidal Anti-Inflammatory Drugs with Low Gastric Ulcerogenic Activity
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- 作者：Naoki Yamakawa ; Shintaro Suemasu ; Yoshinari Okamoto ; Ken-ichiro Tanaka ; Tomoaki Ishihara ; Teita Asano ; Keishi Miyata ; Masami Otsuka ; Tohru Mizushima
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：June 14, 2012
- 年：2012
- 卷：55
- 期：11
- 页码：5143-5150
- 全文大小：389K
- 年卷期：v.55,no.11(June 14, 2012)
- ISSN：1520-4804
文摘
We previously reported that 2-fluoroloxoprofen has lower gastric ulcerogenic activity than loxoprofen, a nonsteroidal anti-inflammatory drug (NSAID) without selectivity for COX-2. We synthesized derivatives of 2-fluoroloxoprofen and studied their properties. Compared to 2-fluoroloxoprofen, one derivative, 11a, exhibited higher anti-inflammatory activity and an equivalent ulcerogenic effect. These results suggest that 11a could be therapeutically beneficial for use as an NSAID.