2. Academic Validation
  3. Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners

Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners

  • Bioorg Med Chem Lett. 2010 Jun 1;20(11):3420-5. doi: 10.1016/j.bmcl.2010.04.006.
Min Ju Kim 1,  Junwon Lee,  Suk Youn Kang,  Sung-Han Lee,  Eun-Jung Son,  Myung Eun Jung,  Suk Ho Lee,  Kwang-Seop Song,  MinWoo Lee,  Ho-Kyun Han,  Jeongmin Kim,  Jinhwa Lee
Affiliations

Affiliation

  • 1 Central Research Laboratories, Green Cross Corporation, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
PMID: 20434909 DOI: 10.1016/j.bmcl.2010.04.006
Abstract

Novel C-aryl glucoside SGLT2 inhibitors containing pyridazine motif were designed and synthesized for biological evaluation. Among the compounds tested, pyridazine containing methylthio moiety 22l or thiadiazole ring 22ah showed the best in vitro inhibitory activities in this series (IC(50)=13.4, 11.4nM, respectively) against SGLT2 to date. Subsequently, compound 22l exhibited reasonable urinary glucose excretion and glucosuria in normal SD rats, thereby demonstrating that this pyridazine series possesses both in vitro SGLT2 inhibition and in vivo efficacy, albeit to a lower degree.

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