Ren, Shen published the artcileDesign, synthesis and evaluation of 2,2-dimethyl-1,3-dioxolane-4,5-dicarboxylic acid derivatives as neuroimmunophilin ligands, Quality Control of 101-98-4, the publication is Zhongguo Yaowu Huaxue Zazhi (2007), 17(1), 1-7, 12, database is CAplus.
A method for the synthesis of the title compounds is reported here. Both, the sequence and conformation of the FK506-binding site in FKBPs (FK506 binding proteins) family are highly conserved. According to this characteristic of FKBPs and the structural feature of ligands binding to FKBP12, CADD (computer-aided drug design) was employed to design and virtually screen novel 2,2-dimethyl-1,3-dioxolane-4,5-5-dicarboxylic acid derivatives These compounds were synthesized by a liquid-phase synthetic method. A model of chick embryos dorsal root ganglion (DRG) cultures free of serum and a model of NG108-15 cell injured by H2O2 were applied to evaluate neurotropic activity of these target compounds Thus, 27 target compounds were synthesized. In cultured chick DRGs, N-[[(4R,5R)-5-[[(cyclohexyl)amino]carbonyl]-2,2-dimethyl-1,3-dioxolan-4-yl]carbonyl]-L-aspartic acid di-Et ester produced a little neurotrophic effect and promoted neurite outgrowth in vitro. In the model of H2O2-induced NG108 cell damage, N-[[(4R,5R)-2,2-dimethyl-5-[[(phenylmethyl)amino]carbonyl]-1,3-dioxolan-4-yl]carbonyl]-L-serine Et ester showed a significantly protective effect on an NG 108 cell.
Zhongguo Yaowu Huaxue Zazhi published new progress about 101-98-4. 101-98-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Alcohol, name is 2-(Benzyl(methyl)amino)ethanol, and the molecular formula is C10H15NO, Quality Control of 101-98-4.
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