Synthesis and Biological Evaluation of Thiophene-C-glucosides as Sodium-Dependent Glucose Cotransporter 2 Inhibitors

The synthesis and structure–activity relationship (SAR) of thiophene-C-glucosides have been explored, and the human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitory activities and rat urinary glucose excretion (UGE) effects of 3a–f were evaluated. As a result, they showed good hSGLT2 inh...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 2013/10/01, Vol.61(10), pp.1037-1043
Hauptverfasser:	Sakamaki, Shigeki, Kawanishi, Eiji, Koga, Yuichi, Yamamoto, Yasuo, Kuriyama, Chiaki, Matsushita, Yasuaki, Ueta, Kiichiro, Nomura, Sumihiro
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Body Weight - drug effects CHO Cells Cricetinae Cricetulus glucal-boronate Glucose - metabolism Glucosides - chemical synthesis Glucosides - chemistry Glucosides - pharmacology Humans Hypoglycemic Agents - chemical synthesis Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Male Rats Rats, Sprague-Dawley sodium-dependent glucose cotransporter Sodium-Glucose Transporter 2 - metabolism Sodium-Glucose Transporter 2 Inhibitors Sorbitol - analogs & derivatives Sorbitol - chemical synthesis Sorbitol - chemistry Sorbitol - pharmacology Structure-Activity Relationship thiophene-C-glucoside Thiophenes - chemistry
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Zusammenfassung:	The synthesis and structure–activity relationship (SAR) of thiophene-C-glucosides have been explored, and the human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitory activities and rat urinary glucose excretion (UGE) effects of 3a–f were evaluated. As a result, they showed good hSGLT2 inhibitory activities and rat UGE effects. In particular, the chlorothiophene derivative 3f showed remarkable inhibitory activity against hSGLT2.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.c13-00407