83599-40-0Relevant articles and documents
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
Yamakawa, Naoki,Suemasu, Shintaro,Matoyama, Masaaki,Kimoto, Ayumi,Takeda, Miho,Tanaka, Ken-Ichiro,Ishihara, Tomoaki,Katsu, Takashi,Okamoto, Yoshinari,Otsuka, Masami,Mizushima, Tohru
scheme or table, p. 7879 - 7882 (2011/02/22)
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.
Reduction of drug ketones by dihydrodiol dehydrogenases, carbonyl reductase and aldehyde reductase of human liver
Ohara, Hirotami,Miyabe, Yoshiyuki,Deyashiki, Yoshihiro,Matsuura, Kazuya,Hara, Akira
, p. 221 - 227 (2007/10/03)
In this study, we compared the enzymatic reduction of 10 drugs with a ketone group by homogeneous carbonyl reductase, aldehyde reductase and three dihydrodiol dehydrogenases of human liver cytosol. At least one and in some cases all of the three dihydrodi
Synthesis of the eight possible optically active isomers of 2-[4-(2-hydroxycyclopentylmethyl)phenyl]propionic acid
Naruto,Terada
, p. 4319 - 4323 (2007/10/02)
A recently synthesized compound, (±)-2-[4-(2-oxocyclopentylmethyl)phenyl]propionic acid, had good anti-inflammatory and analgesic activities. One of the metabolites of this compound showed more potent prostaglandin synthetase inhibitory activity than the
