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

Naoki Yamakawa, Shintaro Suemasu, Masaaki Matoyama, Ayumi Kimoto, Miho Takeda, Ken Ichiro Tanaka, Tomoaki Ishihara, Takashi Katsu, Yoshinari Okamoto, Masami Otsuka, Tohru Mizushima

研究成果: Article

16 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)7879-7882
ページ数4
ジャーナルJournal of Medicinal Chemistry
53
21
DOI
出版ステータスPublished - 2010 11 11

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

フィンガープリント 「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」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

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