Ghisaidoobe, Amar T.; van den Berg, Richard J. B. H. N.; Butt, Saleem S.; Strijland, Anneke; Donker-Koopman, Wilma E.; Scheij, Saskia; van den Nieuwendijk, Adrianus M. C. H.; Koomen, Gerrit-Jan; van Loevezijn, Arnold; Leemhuis, Mark; Wennekes, Tom; van der Stelt, Mario; van der Marel, Gijsbert A.; van Boeckel, Constant A. A.; Aerts, Johannes M. F. G.; Overkleeft, Herman S. published the artcile< Identification and Development of Biphenyl Substituted Iminosugars as Improved Dual Glucosylceramide Synthase/Neutral Glucosylceramidase Inhibitors>, Synthetic Route of 112-63-0, the main research area is biphenyl iminosugar preparation glucosylceramide synthase glucosylceramidase inhibitor.
This work details the evaluation of a number of N-alkylated deoxynojirimycin derivatives on their merits as dual glucosylceramide synthase/neutral glucosylceramidase inhibitors. Building on the previous work, the authors synthesized a series of D-gluco and L-ido-configured iminosugars N-modified with a variety of hydrophobic functional groups. The authors found that iminosugars featuring N-pentyloxymethylaryl substituents are considerably more potent inhibitors of glucosylceramide synthase than their aliphatic counterparts. In a next optimization round, the authors explored a series of biphenyl-substituted iminosugars of both configurations (D-gluco and L-ido) with the aim to introduce structural features known to confer metabolic stability to drug-like mols. From these series, two sets of mols. emerge as lead series for further profiling. Biphenyl-substituted L-ido-configured deoxynojirimycin derivatives are selective for glucosylceramidase and the nonlysosomal glucosylceramidase, and the authors consider these as leads for the treatment of neuropathol. lysosomal storage disorders. Their D-gluco-counterparts are also potent inhibitors of intestinal glycosidases, and because of this characteristic, the authors regard these as the prime candidates for type 2 diabetes therapeutics.
Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Synthetic Route of 112-63-0.
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