Pyrimidinylmethylphenyl glucoside as novel C-aryl glucoside SGLT2 inhibitors

Junwon Lee; Jong Yup Kim; Jungsub Choi; Sung-Han Lee; Jeongmin Kim; Jinhwa Lee

doi:10.1016/j.bmcl.2010.09.103

Pyrimidinylmethylphenyl glucoside as novel C-aryl glucoside SGLT2 inhibitors

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7046-9. doi: 10.1016/j.bmcl.2010.09.103. Epub 2010 Sep 29.

Authors

Junwon Lee¹, Jong Yup Kim, Jungsub Choi, Sung-Han Lee, Jeongmin Kim, Jinhwa Lee

Affiliation

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

PMID: 20952196
DOI: 10.1016/j.bmcl.2010.09.103

Abstract

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).

MeSH terms

Animals
Glucosides / chemistry*
Glucosides / pharmacology*
Humans
Hypoglycemic Agents / pharmacology
Inhibitory Concentration 50
Mice
Pyrimidines / chemistry
Pyrimidines / pharmacology
Sodium-Glucose Transporter 2 Inhibitors*
Structure-Activity Relationship
Xenograft Model Antitumor Assays

Substances

Glucosides
Hypoglycemic Agents
Pyrimidines
Sodium-Glucose Transporter 2 Inhibitors