Amplification of the inhibitory activity of miglitol by monofluorination

Author:

Prell Erik,Csuk René

Publisher

Elsevier BV

Subject

Organic Chemistry,Clinical Biochemistry,Drug Discovery,Pharmaceutical Science,Molecular Biology,Molecular Medicine,Biochemistry

Reference10 articles.

1. Miglitol suppresses the postprandial increase in interleukin 6 and enhances active glucagon-like peptide 1 secretion in viscerally obese subjects

2. Mahuran, D. J.; Tropak, M. B.; Buttner, E. D.; Blanchard, J. E.; Brown, E. D. U.S. Patent 2009075960 A1, 2009; Chem. Abstr. 2009, 150, 345565.

3. Visualization was performed using the CAChe 4.0 software from Oxford molecular; structural superimpositions were conducted using the SWISS PDB and Cn3D free software; docking simulation were run using a modified algorithm. GOLD (Jones, G.; Willett, P.; Glen, R. C.; Leach, A. R.; Taylor, R. J. Mol. Biol. 1997, 267, 727). Crystal structure data were obtained from the PDB structures 3D3I and 2JKE: Kurakata, Y.; Uechi, A.; Yoshida, H.; Kamitori, S.; Sakano, Y.; Nishikawa, A.; Tonozuka, T. J. Biol. Chem. 2008, 381, 116 and Gloster, T. M.; Turkenburg, J. P.; Potts, J. R.; Henrisat, B.; Davies, G. J. Chem. Biol. 2008, 15, 1058; for comparative 3-D-QSAR studies: Saqib, U.; Siddiqi, M. I. Int. J. Integr. Biol. 2009, 5(1), 13; a similar in-silico approach—although on HIV-1 integrase inhibitors—has been described by Savarino: Savarino, A. Retrovirology 2007, 4, 21.

4. Use of Trifluoromethanesulfonic Acid in Fischer Glycosylations

5. Synthesis of (+)-1,5-dideoxy-1,5-imino-d-galactitol, a potent α-d-galactosidase inhibitor

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