Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
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DOI：
10.1021/jm101116s
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发表时间：
2010-11
影响因子：
7.3
通讯作者：
N. Yamakawa;Shintaro Suemasu;Masaaki Matoyama;Ayumi Kimoto;Miho Takeda;Ken-ichiro Tanaka;T. Ishihara;T. Katsu;Yoshinari Okamoto;M. Otsuka;T. Mizushima
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文献类型：
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作者：
N. Yamakawa;Shintaro Suemasu;Masaaki Matoyama;Ayumi Kimoto;Miho Takeda;Ken-ichiro Tanaka;T. Ishihara;T. Katsu;Yoshinari Okamoto;M. Otsuka;T. Mizushima
我们之前提出非甾体抗炎药的膜透化活性与非甾体抗炎药诱导的胃损伤有关。我们在这里合成的洛索洛芬衍生物，具有较低的膜透化活性比其他非甾体抗炎药。与洛索洛芬相比，衍生物10a和10b具有较低的膜透化活性，并且它们的口服给药产生较少的胃损伤，但显示出等同的抗炎作用。这些结果表明，10a和10b作为更安全的NSAID可能是治疗上有益的。
We previously proposed that membrane permeabilization activity of NSAIDs is involved in NSAID-induced gastric lesions. We here synthesized derivatives of loxoprofen that have lower membrane permeabilization activity than other NSAIDs. Compared to loxoprofen, the derivatives 10a and 10b have lower membrane permeabilization activity and their oral administration produced fewer gastric lesions but showed an equivalent anti-inflammatory effect. These results suggest that 10a and 10b are likely to be therapeutically beneficial as safer NSAIDs.