1310460-70-8Relevant articles and documents
Hydrophobic substituents increase the potency of salacinol, a potent α-glucosidase inhibitor from Ayurvedic traditional medicine ‘Salacia’
Tanabe, Genzoh,Xie, Weijia,Balakishan, Gorre,Amer, Mumen F.A.,Tsutsui, Nozomi,Takemura, Haruka,Nakamura, Shinya,Akaki, Junji,Ninomiya, Kiyofumi,Morikawa, Toshio,Nakanishi, Isao,Muraoka, Osamu
, p. 3705 - 3715 (2016/07/20)
Using an in silico method, seven analogs bearing hydrophobic substituents (8a: Me, 8b: Et, 8c: n-Pent, 8d: n-Hept, 8e: n-Tridec, 8f: isoBu and 8g: neoPent) at the 3′-O-position in salacinol (1), a highly potent natural α-glucosidase inhibitor from Ayurvedic traditional medicine ‘Salacia’, were designed and synthesized. In order to verify the computational SAR assessments, their α-glucosidase inhibitory activities were evaluated in vitro. All analogs (8a–8g) exhibited an equal or considerably higher level of inhibitory activity against rat small intestinal α-glucosidases compared with the original sulfonate (1), and were as potent as or higher in potency than the clinically used anti-diabetics, voglibose, acarbose or miglitol. Their activities against human maltase exhibited good relationships to the results obtained with enzymes of rat origin. Among the designed compounds, the one with a 3′-O-neopentyl moiety (8g) was most potent, with an approximately ten fold increase in activity against human maltase compared to 1.
CYCLIC SULFONIUM SALT, PROCESS FOR PRODUCTION OF SAME, AND alpha-GLUCOSIDASE INHIBITOR COMPRISING SAME
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Paragraph 0090-0092, (2014/01/08)
Provided is a novel cyclic sulfonium salt compound which is useful for the prevention or treatment of diabetes and the like. The present invention relates to a novel cyclic sulfonium salt compound represented by general formula (I) or (II), an isomer or solvate of the compound, or a pharmaceutically acceptable salt of the compound or the isomer or solvate. The present invention also relates to an α-glucosidase inhibitor, a pharmaceutical composition for preventing or treating diabetes, and an anti-diabetes food, each of which comprises the compound represented by general formula (I) or (II) and the like.