Cheng, Wei-Chieh published the artcileRapid modifications of N-substitution in imino-sugars: Development of new β-glucocerebrosidase inhibitors and pharmacological chaperones for Gaucher disease, Product Details of C8H7ClO3, the publication is Bioorganic & Medicinal Chemistry (2013), 21(17), 5021-5028, database is CAplus and MEDLINE.
The rapid discovery of β-glucocerebrosidase (GCase) inhibitors and pharmacol. chaperones for Gaucher disease is described. The N-aminobutyl DNJ-based iminosugar was synthesized and conjugating with a variety of carboxylic acids to generate a N-diversely substituted iminosugar-based library. Several members of this library were found to be nanomolar-range inhibitors of GCase; the inhibition constant Ki of the most potent was found to be 71 nM. Although these new mols. showed reasonable chaperoning activity (1.5- to 1.9-fold) in the N370S fibroblast of Gaucher patient-derived cell line, this was accompanies by a concomitant decrease in the cellular α-glucosidase activity, which might limit their further therapeutic potential. Next, newly developed N-substituents were assembled with pyrrolidine-based scaffolds to generate new mols. for further evaluation. The new 2,5-dideoxy-2,5-imino-D-mannitol (DMDP)-based iminosugar 22 was found to exhibit a satisfactory chaperoning activity to enhance GCase activity by 2.2-fold in Gaucher N370S cell line, without impairment of cellular α-glucosidase activity.
Bioorganic & Medicinal Chemistry published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Product Details of C8H7ClO3.
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