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
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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DOI：
10.1021/jm300049g
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发表时间：
2012-06-14
影响因子：
7.3
通讯作者：
Mizushima, Tohru
中科院分区：
文献类型：
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作者：
Yamakawa, Naoki;Suemasu, Shintaro;Mizushima, Tohru
我们先前报道，2-氟氧洛芬的胃溃疡形成活性低于洛索洛芬，后者是一种对COX-2没有选择性的非类固醇抗炎药(NSAID)。我们合成了2-氟氧洛芬的衍生物，并研究了它们的性质。与2-氟氧洛芬相比，1个1a的衍生物具有更高的抗炎活性和相当的溃疡形成作用。这些结果表明，11a作为一种非甾体抗炎药在治疗上可能是有益的。
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, 1 la, exhibited higher anti-inflammatory activity and an equivalent ulcerogenic effect. These results suggest that 11a could be therapeutically beneficial for use as an NSAID.