6640-09-1Relevant articles and documents
AROMATIC RING DERIVATIVE AS IMMUNOREGULATION AND PREPARATION METHOD AND APPLICATION OF AROMATIC RING DERIVATIVE
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Paragraph 0064-0065, (2021/10/15)
Relating to a compound represented by formula (I) and a pharmaceutically acceptable salt of the compound, and an application of the compound as an S1P1 agonist.
Structure-based design and biological evaluation of novel 2-(indol-2-yl) thiazole derivatives as xanthine oxidase inhibitors
Song, Jeong Uk,Jang, Jae Wan,Kim, Tae Hun,Park, Heuisul,Park, Wan Su,Jung, Sang-Hun,Kim, Geun Tae
, p. 950 - 954 (2016/05/24)
Inhibition of xanthine oxidase (XO) has obviously been a central concept for controlling hyperuricemia, which causes serious and painful inflammatory arthritis disease such as gout. We discovered a series of novel 2-(indol-2-yl)thiazole derivatives as XO inhibitors at the level of nanomolar activity. Structure-guided design using molecular modeling program (Accelrys Software program) provided an excellent basis for optimization of 2-(indol-2-yl)thiazole compounds. Structure-activity relationship indicated that hydrophobic alkoxy group (isopropoxy, cyclopentoxy) at 5-position and hydrogen binding acceptor (NO2, CN) at 7-position of indole ring appear as critical functional groups. Among the compounds, 2-(7-nitro-5-isopropoxy-indol-2-yl)-4-methylthiazole-5-carboxylic acid (9m) exhibits the most potent XO inhibitory activity (IC50value: 5.1 nM) and the excellent uric acid lowering activity in potassium oxonate induced hyperuricemic rat model.
A simple method for chemoselective phenol alkylation
Liu, Pingli,Huang, Liang,Faul, Margaret M.
, p. 7380 - 7382 (2008/03/13)
A simple and effective method for chemoselective alkylation of phenol over carboxylic acid using a 40% aqueous solution of tetrabutylphosphonium hydroxide that affords the desired phenyl ethers in 82-99% yield is described.
