Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Yin, Fei, once mentioned the application of 615-05-4, Name is 4-Methoxybenzene-1,3-diamine, molecular formula is C7H10N2O, molecular weight is 138.17, MDL number is MFCD00007803, category is amides-buliding-blocks. Now introduce a scientific discovery about this category, Recommanded Product: 615-05-4.
The affinity of a series of iminosugar-based inhibitors exhibiting various ring sizes toward Hex A and their essential interactions with the enzyme active site were investigated. All the Hex A-inhibiting iminosugars tested formed hydrogen bonds with Arg178, Asp322, Tyr421 and Glu462 and had the favorable cation-pi interaction with Trp460. Among them, DMDP amide (6) proved to be the most potent competitive inhibitor with a K-i value of 0.041 mu M. We analyzed the dynamic properties of both DMDP amide (6) and DNJNAc (1) in aqueous solution using molecular dynamics (MD) calculations; the distance of the interaction between Asp322 and 3-OH and Glu323 and 6-OH was important for stable interactions with Hex A, reducing fluctuations in the plasticity of the active site. DMDP amide (6) dose-dependently increased intracellular Hex A activity in the G269S mutant cells and restored Hex A activity up to approximately 43% of the wild type level; this effect clearly exceeded the border line treatment for Tay-Sachs disease, which is regarded as 10-15% of the wild type level. This is a significantly greater effect than that of pyrimethamine, which is currently in Phase 2 clinical trials. DMDP amide (6), therefore, represents a new promising pharmacological chaperone candidate for the treatment of Tay-Sachs disease.
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Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics