|
|||||
|
|
N-glucosides as human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitors |
|
| Authors: | Yasuo Yamamoto Eiji Kawanishi Yuichi Koga Shigeki Sakamaki Toshiaki Sakamoto Kiichiro Ueta Yasuaki Matsushita Chiaki Kuriyama Minoru Tsuda-Tsukimoto Sumihiro Nomura |
| Institution: | 1. Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation, 2-2-50 Kawagishi, Toda, Saitama 335-8505, Japan;2. Pharmacology Research Laboratories, Mitsubishi Tanabe Pharma Corporation, 2-2-50 Kawagishi, Toda, Saitama 335-8505, Japan;3. DMPK Research Laboratories, Mitsubishi Tanabe Pharma Corporation, 2-2-50 Kawagishi, Toda, Saitama 335-8505, Japan |
| Abstract: | Inhibition of renal sodium-dependent glucose cotransporter 2 (SGLT2) increases urinary glucose excretion (UGE), and thus reduces blood glucose levels in hyperglycemia. A series of N-glucosides was synthesized for biological evaluation as human SGLT2 (hSGLT2) inhibitors. Among these compounds, N-glucoside 9d possessing an indole core structure showed good in vitro activity (IC50 = 7.1 nM against hSGLT2). Furthermore, 9d exhibited favorable in vivo potency with regard to UGE in rats based on good pharmacokinetic profiles. |
| Keywords: | SGLT2 Sodium-dependent glucose cotransporter Diabetes Glucoside N-glucoside |
| 本文献已被 ScienceDirect 等数据库收录！ | |