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 the compounds assayed, pyrimidine containing methylthio moiety 11 g demonstrated the best in vitro inhibitory activity against SGLT2 in this series to date (IC(50)=10.7 nM).
Lee
Junwon
J
Research Center, Green Cross Corporation, Giheung-Gu, Yongin, Gyeonggi-Do, Republic of Korea.
Kim
Jong Yup
JY
Choi
Jungsub
J
Lee
Sung-Han
SH
Kim
Jeongmin
J
Lee
Jinhwa
J
D000818:Animals; D005960:Glucosides / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051379:Mice; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
D005960:Glucosides; D007004:Hypoglycemic Agents; D011743:Pyrimidines; D000077203:Sodium-Glucose Transporter 2 Inhibitors