Synthesis and biological evaluation of novel C-aryl d-glucofuranosides as sodium-dependent glucose co-transporter 2 inhibitors.
Novel C-aryl-d-glucofuranosides were synthesized and evaluated for their capacity to inhibit human sodium-dependent glucose co-transporter 2 (hSGLT2) and hSGLT1. Compound 21q demonstrated the best in vitro inhibitory activity against SGLT2 in this series (EC50=0.62μM).
School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan.
Tzung-Sheng
TS
Lin
Ya-Wen
YW
Liw
Jen-Shin
JS
Song
Tsung-Chih
TC
Hsieh
Hsien-Wei
HW
Yeh
Lih-Ching
LC
Hsu
Chun-Jung
CJ
Lin
Szu-Huei
SH
Wu
Pi-Hui
PH
Liang
D000818:Animals; D001559:Benzhydryl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D005959:Glucosidases / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D005960:Glucosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D010695:Phlorhizin / Q000737:chemistry; D011485:Protein Binding; D051269:Sodium-Glucose Transporter 1 / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D051297:Sodium-Glucose Transporter 2 / Q000235:genetics / Q000378:metabolism; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013329:Structure-Activity Relationship
C000588457:1,4-anhydro-1-(4-chloro-5-(4-ethylbenzyl)-2-methoxyphenyl)glucitol; D001559:Benzhydryl Compounds; D005960:Glucosides; D051269:Sodium-Glucose Transporter 1; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D010695:Phlorhizin; D005959:Glucosidases
Antidiabetics; Glucofuranosides; SGLT