Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: 1,3,4-Thiadiazolylmethylphenyl glucoside congeners |
| |
Authors: | Junwon Lee Sung-Han Lee Hee Jeong Seo Eun-Jung Son Suk Ho Lee Myung Eun Jung MinWoo Lee Ho-Kyun Han Jeongmin Kim Jahyo Kang Jinhwa Lee |
| |
Institution: | 1. Central Research Laboratories, Green Cross Corporation, 303 Bojeong-Dong, Giheung-Gu, Yongin, Gyeonggi-Do 446-770, Republic of Korea;2. Department of Chemistry, Sogang University, 1 Shinsu-Dong, Mapo-Gu, Seoul 121-742, Republic of Korea |
| |
Abstract: | Novel C-aryl glucoside SGLT2 inhibitors containing 1,3,4-thiadiazole moieties were designed and synthesized. Among the compounds tested, biaryl-type compounds containing pyrazine 59, 2-furan 61, and 3-thiophene 71 showed the best in vitro inhibitory activities to date (IC50 = 3.51–7.03 nM) against SGLT2. A selected compound 61, demonstrated reasonable blood glucose-lowering effects, indicating that the information obtained from the SAR studies in this 1,3,4-thiadiazolylmethylphenyl glucoside series might help to design more active SGLT2 inhibitors that are structurally related. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|