Pyrimidinylmethylphenyl glucoside as novel C-aryl glucoside SGLT2 inhibitors

Novel C-aryl glucoside SGLT2 inhibitors containing pyrimidine motif were designed and synthesized for biological evaluation. Among various analogs tested, methylthiopyrimidine 11g demonstrated best in vitro activity against hSGLT2 in this series to date. Novel C-aryl glucoside SGLT2 inhibitors conta...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.7046-7049
Hauptverfasser:	Lee, Junwon, Kim, Jong Yup, Choi, Jungsub, Lee, Sung-Han, Kim, Jeongmin, Lee, Jinhwa
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Dapagliflozin Diabetes General and cellular metabolism. Vitamins Glucoside Glucosides - chemistry Glucosides - pharmacology Humans Hypoglycemic Agents - pharmacology Inhibitory Concentration 50 Medical sciences Mice Pharmacology. Drug treatments Pyrimidine Pyrimidines - chemistry Pyrimidines - pharmacology SGLT Sodium-Glucose Transporter 2 - antagonists & inhibitors Structure-Activity Relationship Xenograft Model Antitumor Assays
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Zusammenfassung:	Novel C-aryl glucoside SGLT2 inhibitors containing pyrimidine motif were designed and synthesized for biological evaluation. Among various analogs tested, methylthiopyrimidine 11g demonstrated best in vitro activity against hSGLT2 in this series to date. Novel C-aryl glucoside SGLT2 inhibitors containing pyrimidine motif were designed and synthesized for biological evaluation. Among the compounds assayed, pyrimidine containing methylthio moiety 11g demonstrated the best in vitro inhibitory activity against SGLT2 in this series to date (IC 50 = 10.7 nM).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.09.103