Song, Jeong Uk published the artcileDesign and synthesis of novel 2-(indol-5-yl)thiazole derivatives as xanthine oxidase inhibitors, Category: bromides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(6), 1254-1258, database is CAplus and MEDLINE.
Xanthine oxidase (XO) inhibitors were widely used for the treatment of gout. Indole rings are frequently used as active scaffold in designing inhibitors for enzymes. Herein, the authors describe the structure-activity relation for novel xanthine oxidase inhibitors based on indole scaffold. A series of novel tri-substituted 2-(indol-5-yl)thiazole derivatives were synthesized, and their in vitro inhibitory activities against xanthine oxidase and in vivo efficacy lowering uric acid level in blood were measured. Among them, 2-(3-cyano-2-isopropylindol-5-yl)-4-methylthiazole-5-carboxylic acid exhibits the most potent XO inhibitory activity (IC50 value: 3.5 nM) and the excellent plasma uric acid lowering activity. Study of structure activity relation indicated that hydrophobic moiety (e.g., isopropyl) at 1-position and electron withdrawing group (e.g., CN) at 3-position of indole ring and small hydrophobic group (CH3) at 4-position of the thiazole ring enhanced the XO inhibitory activity. Hydrophobic substitution such as iso-Pr at 1-position of the indole moiety without any substitution at 2-position has an essential role for enhancing bioavailability and therefore for high in vivo efficacy.
Bioorganic & Medicinal Chemistry Letters published new progress about 16523-02-7. 16523-02-7 belongs to bromides-buliding-blocks, auxiliary class Bromide,Sulfone,Aliphatic hydrocarbon chain, name is 2-Bromoethyl Methyl Sulfone, and the molecular formula is C2H2N4O2, Category: bromides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary