78304-52-6Relevant academic research and scientific papers
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.
INDOLYLS. SYNTHESIS OF DI(5-INDOLYL) OXIDE
Samsoniya, Sh. A.,Tabidze, D. M.,Suvorov, N. N.
, p. 45 - 49 (2007/10/02)
Bis(2-carbethoxy-5-indolyl) oxide was obtained by cyclization of ethyl pyruvate 4,4'-diphenyloxydihydrazone. 5-Phenoxy-2-carbethoxyindole was also isolated from the reaction products.Saponification of these sters gave the corresponding acids, the thermal
