On October 31, 2020, Liang, Xiao; Fu, Huansheng; Xiao, Peng; Fang, Hao; Hou, Xuben published an article.Category: bromides-buliding-blocks The title of the article was Design, synthesis and biological evaluation of imidazolidine-2,4-dione and 2-thioxothiazolidin-4-one derivatives as lymphoid-specific tyrosine phosphatase inhibitors. And the article contained the following:
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. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Category: bromides-buliding-blocks
The Article related to thioxothiazolidinone preparation docking lymphoid tyrosine phosphatase inhibitor autoimmunity, imidazolidinedione preparation diastereoselective docking lymphoid tyrosine phosphatase inhibitor autoimmunity, autoimmune diseases, inhibitor, lymphoid-specific tyrosine phosphatase and other aspects.Category: bromides-buliding-blocks
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary