Liang, Xiao’s team published research in Bioorganic Chemistry in 2020-10-31 | 10574-69-3

Bioorganic Chemistry published new progress about Aralkyl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Name: 3-Benzyl-2-thioxothiazolidin-4-one.

Liang, Xiao; Fu, Huansheng; Xiao, Peng; Fang, Hao; Hou, Xuben published the artcile< Design, synthesis and biological evaluation of imidazolidine-2,4-dione and 2-thioxothiazolidin-4-one derivatives as lymphoid-specific tyrosine phosphatase inhibitors>, Name: 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is thioxothiazolidinone preparation docking lymphoid tyrosine phosphatase inhibitor autoimmunity; imidazolidinedione preparation diastereoselective docking lymphoid tyrosine phosphatase inhibitor autoimmunity; Autoimmune diseases; Inhibitor; Lymphoid-specific tyrosine phosphatase.

Synthesized imidazolidine-2,4-dione derivatives I [R = carboxymethyl, Ph, benzyl, (4-carboxyphenyl)methyl, (4-phenylphenyl)methyl] and 2-thioxothiazolidin-4-one derivatives II (R1 = Bu, cyclohexyl, 2-chlorophenyl, thiazol-2-yl, etc.; R2 = carboxy, 4-carboxyphenyl, 2-carboxyeth-1-en-1-yl, etc.) as new LYP inhibitors were designed. Among them, the cinnamic acids-based inhibitors II [R1 = 2-methoxyphenyl, R2 = ((4-((1E)-2-carboxyeth-1-en-1-yl)phenyl)methyl)oxidanyl; R1 = 4-chlorophenyl, R2 = ((4-((1E)-2-carboxyeth-1-en-1-yl)phenyl)methyl)oxidanyl (III)] displayed good LYP inhibitory activities (IC50 = 2.85-6.95μM). Especially, the most potent inhibitor III was identified as competitive inhibitor (Ki = 1.09μM) and bind LYP reversibly. Meanwhile, III exhibited better selectivity over other phosphatases than known LYP inhibitor A15. Furthermore, compound III could regulate TCR associated signaling pathway in Jurkat T cell.

Bioorganic Chemistry published new progress about Aralkyl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Name: 3-Benzyl-2-thioxothiazolidin-4-one.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica