The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Methyl 5-methoxyindole-2-carboxylate( cas:67929-86-6 ) is researched.Formula: C11H11NO3.Song, Jeong Uk; Jang, Jae Wan; Kim, Tae Hun; Park, Heuisul; Park, Wan Su; Jung, Sang-Hun; Kim, Geun Tae published the article 《Structure-based design and biological evaluation of novel 2-(indol-2-yl) thiazole derivatives as xanthine oxidase inhibitors》 about this compound( cas:67929-86-6 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: structure indolyl thiazole derivative preparation xanthine oxidase antiinflammatory gout; 2-(Indol-2-yl)thiazole; Hyperuricemia; Molecular modeling; Structure–activity relationship; Xanthine oxidase inhibitors. Let’s learn more about this compound (cas:67929-86-6).
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 mol. 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 (IC50 value: 5.1 nM) and the excellent uric acid lowering activity in potassium oxonate induced hyperuricemic rat model.
Here is a brief introduction to this compound(67929-86-6)Formula: C11H11NO3, if you want to know about other compounds related to this compound(67929-86-6), you can read my other articles.
Reference:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem