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Title 

A novel competitive class of alpha-glucosidase inhibitors: (E)-1-phenyl-3-(4-styrylphenyl)urea derivatives

 

신규한 알파 글루코시다아제 경쟁적 저해제: (E)-1-Phenyl-3-(4-styrylphenyl)urea 유도체

Authors 

J Y KimJ W LeeY S KimY LeeYoung Bae RyuS KimH W RyuM J Curtis-LongK W LeeWoo Song LeeK H Park

Publisher 

Wiley-Blackwell

Issue Date 

2010

Citation 

ChemBioChem, vol. 11, no. 15, pp. 2125-2131

Abstract 

Competitive glycosidase inhibitors are generally sugar mimics that are costly and tedious to obtain because they require challenging and elongated chemical synthesis, which must be stereo- and regiocontrolled. Here, we show that readily accessible achiral (E)-1-phenyl-3-(4-strylphenyl)ureas are potent competitive α-glucosidase inhibitors. A systematic synthesis study shows that the 1-phenyl moiety on the urea is critical for ensuring competitive inhibition, and substituents on both terminal phenyl groups contribute to inhibition potency. The most potent inhibitor, compound 12 (IC(50)=8.4 μM, K(i)=3.2 μM), manifested a simple slow-binding inhibition profile for α-glucosidase with the kinetic parameters k(3)=0.005256 μM(-1)?min(-1), k(4)=0.003024 min(-1), and K(i)(app) =0.5753 μM.

ISSN 

1439-4227

Link 

http://dx.doi.org/10.1002/cbic.201000376.

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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