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Bioorg Med Chem Lett. 2011 Jun 15;21(12):3759-63. doi: 10.1016/j.bmcl.2011.04.063. Epub 2011 Apr 28.

Glucosides with cyclic diarylpolynoid as novel C-aryl glucoside SGLT2 inhibitors.

Author information

1
Research Center, Green Cross Corporation, Yongin, Gyeonggi-Do, Republic of Korea.

Abstract

Novel C-aryl glucoside SGLT2 inhibitors containing cyclic diarylpolynoid motif were designed and synthesized for biological evaluation. Alkylzinc bromides have been efficiently prepared by the direct insertion of zinc metal into alkyl bromides. The organozinc reagents underwent smooth Pd-catalyzed cross-coupling reactions. Subsequent ring closing metathesis using 2nd generation Grubbs catalyst successfully generated novel class of ansa-compounds. These glucosides with cyclic diarylpolynoids demonstrated moderate in vitro inhibitory activity against SGLT2 in this series to date (IC(50)=59.5-103 nM).

PMID:
21592794
DOI:
10.1016/j.bmcl.2011.04.063
[Indexed for MEDLINE]

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