79219-21-9Relevant academic research and scientific papers
Study on the design, synthesis and structure-activity relationships of new thiosemicarbazone compounds as tyrosinase inhibitors
Song, Senchuan,You, Ao,Chen, Zhiyong,Zhu, Guoxun,Wen, Huan,Song, Huacan,Yi, Wei
, p. 815 - 825 (2017/09/05)
52 Structure-based thiosemicarbazone compounds bearing various substituted-lipophilic part, including substituted-benzaldehyde, substituted-phenylalkan-1-one and their biphenyl-type thiosemicarbazone analogs, were designed, synthesized and evaluated as new tyrosinase inhibitors. The results demonstrated that 22 compounds have potent inhibitory activities against tyrosinase with the IC50 value of lower than 1.0 μM. On the basis of the obtained experimental data, the structure-activity relationships (SARs) were rationally derived. Besides, the inhibition mechanism and the inhibitory kinetics of selected compounds 3d and 6e were investigated, revealing that such type of compounds were belonged to the reversible and competitive tyrosinase inhibitors. To verify the safety of these developed thiosemicarbazone compounds, four randomly selected compounds 3d, 4e, 6a and 9a were also tested in 293T cell line for the evaluation of the cytotoxicity. Interestingly, all these compounds almost did not perform any toxicity to 293T cells even at a high concentration of 1000 μmol/L. Taken together, these results suggested that such compounds could serve as the highly efficient and more safe candidates for the treatment of tyrosinase-related disorders.
5-Aryl-imidazolin-2-ones as a scaffold for potent antioxidant and memory-improving activity
Watanabe, Kazutoshi,Morinaka, Yasuhiro,Hayashi, Yoshio,Shinoda, Masaki,Nishi, Hiroyoshi,Fukushima, Nobuko,Watanabe, Toshiaki,Ishibashi, Akira,Yuki, Satoshi,Tanaka, Masahiko
, p. 1478 - 1483 (2008/09/18)
A series of 5-phenyl-substituted-N-alkyl-imidazolin-2-ones with potent radical-scavenging activity and lipid peroxidation inhibitory activity was synthesized. Many of the compounds showed memory-improving effect in animal models independent of the inhibitory activity on lipid peroxidation.
SYNTHESIS OF ARENES FROM PHENOLS BY COUPLING OF ARYL TRIFLATES WITH ORGANOCOPPER REAGENTS
Mc Murry, John E.,Mohanraj, Subramaniam
, p. 2723 - 2726 (2007/10/02)
Aryl triflates react with higher order mixed cuprates R2Cu(CN)Li2 to produce arenes in good yield.The aryl ring may have either an electron-donating or an electron-withdrawing substituent; the organocuprate may be either primary, secondary, tertiary, aryl, or vinyl.
