C-Aryl glucosides substituted at the 4′-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes
A series of C-aryl glucosides with various substituents at the 4′-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. A series of C-aryl glucosides with various substituents at the 4′-position of the distal aryl ring have been synthesized and eva...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2011-08, Vol.21 (15), p.4465-4470 |
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Hauptverfasser: | , , , , , , , , , , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | A series of
C-aryl glucosides with various substituents at the 4′-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2.
A series of
C-aryl glucosides with various substituents at the 4′-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Introduction of alkyl or alkoxy substituents at the 4′-position was found to improve SGLT2 potency, whereas introduction of a hydrophilic group at this position was deleterious. Compounds with alkoxy-, cycloalkoxy- or cycloalkenyloxy-ethoxy scaffolds exhibited good inhibitory activity and high selectivity toward SGLT2. Selected compounds were investigated for in vivo efficacy. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2011.06.032 |