75436-40-7Relevant articles and documents
Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (2)
Asano, Yasutomi,Kitamura, Shuji,Ohra, Taiichi,Itoh, Fumio,Kajino, Masahiro,Tamura, Tomoko,Kaneko, Manami,Ikeda, Shota,Igata, Hideki,Kawamoto, Tomohiro,Sogabe, Satoshi,Matsumoto, Shin-ichi,Tanaka, Toshimasa,Yamaguchi, Masashi,Kimura, Hiroyuki,Fukumoto, Shoji
, p. 4699 - 4714 (2008/09/21)
3-Metoxycarbonyl isoquinolone derivative 1 has been identified as a potent JNK inhibitor and significantly inhibited cardiac hypertrophy in a rat pressure-overload model. Herein, a series of isoquinolones with an imidazolylmethyl or a pyrazolylmethyl group at the 2-position were designed based on X-ray crystallographic analysis of the complex between the isoquinolone compound and JNK3, as wells as the relationship between compound lipophilicity (log D) and activity in a cell-based assay. The compounds prepared showed potent JNK1 inhibitory activities in a cell-based assay. Among them the isoquinolone derivative possessing 5-[(cyclopropylamino)carbonyl]-1-methyl-1H-pyrazole (16e) exhibited significant anti-hypertrophic activity at doses of more than 1 mg/kg (po) in a pressure-overload model.
LE DIMETHYL ACETAL DU DIAZOACETALDEHYDE : UNENOUVELLE VOIE D'ACCES AUX CYCLOPROPANES ALDEHYDES ET AUX FORMYL PYRAZOLES.
Abdallah, Hassan,Gree, Rene
, p. 2239 - 2242 (2007/10/02)
Diazoacetaldehyde dimethylacetal 1 is a readily accessible and highly reactive 1,3 dipole.Starting from 1, both electrophilic cyclopropanes with an extra aldehyde function and formyl pyrazoles are prepared in high yields.