O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 19, 2009, Pages 5632-5635

  Xu, Baihua ^a,b,c   Lv, Binhua ^a,b,c   Feng, Yan ^b   Xu, Ge ^b   Du, Jiyan ^b   Welihinda, Ajith ^d   Sheng, Zelin ^b   Seed, Brian ^d   Chen, Yuanwei ^a,b  

^a CHENGDU INSTITUTE OF ORGANIC CHEMISTRY   (China)

^b Egret Pharma (Shanghai) Limited   (China)

^c UNIVERSITY OF CHINESE ACADEMY OF SCIENCES   (China)

^d Theracos Inc   (United States)

Author keywords

Glucosides; SGLT; Spiro

Indexed keywords

ANTIDIABETIC AGENT; DAPAGLIFLOZIN; GLUCOSIDE; O SPIRO CARBON GLUCOCOSIDE DERIVATIVE; SODIUM GLUCOSE COTRANSPORTER 1; SODIUM GLUCOSE COTRANSPORTER 2; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG BINDING; DRUG CONCENTRATION; DRUG INHIBITION; DRUG SCREENING; HUMAN; HUMAN CELL; IN VITRO STUDY; STRUCTURE ACTIVITY RELATION;

GLUCOSE; GLUCOSIDES; HUMANS; SODIUM-GLUCOSE TRANSPORTER 1; SODIUM-GLUCOSE TRANSPORTER 2; SPIRO COMPOUNDS;

EID: 69949089767     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.08.030     Document Type: Article

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26. 50 calculations were performed using nonlinear regression with variable slope. As a reference standard, a derivative of dapagliflozin was routinely included in the assays. In 26 independent evaluations, the reference compound inhibited SGLT2 activity by 69.7 ± 9.6% and SGLT1 by 72.7 ± 6.7% at 10 nM and 10 μM, respectively.