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Wan H.-X.,Shanghai Pharmaceutical Holding Co. | Shen J.-K.,Shanghai Pharmaceutical Holding Co. | Shen J.-K.,CAS Shanghai Institute of Materia Medica
Yaoxue Xuebao | Year: 2012

Sodium-glucose co-transporters are a family of glucose transporter found in the intestinal mucosa of the small intestine (SGLT-2) and the proximal tubule of the nephron (SGLT-1 and SGLT-2). They contribute to renal glucose reabsorption and most of renal glucose (about 90%) is reabsorbed by SGLT-2 located in the proximal renal tubule. Selectively inhibiting activity of SGLT-2 is an innovative therapeutic strategy for treatment of type 2 diabetes by enhancing urinary glucose excretion from the body. Therefore SGLT-2 inhibitors are considered to be potential antidiabetic drugs with an unique mechanism. This review will highlight some recent advances and structure-activity relationships in the discovery and development of SGLT-2 inhibitors including O-glycoside, C-glycoside, C, O-spiro glycoside and non glycosides.

Yu J.,Shanghai Pharmaceutical Holding Co. | Liu H.,Shanghai Pharmaceutical Holding Co. | Xia G.,Shanghai Pharmaceutical Holding Co. | Xia G.,CAS Shanghai Institute of Materia Medica | And 14 more authors.
ACS Medicinal Chemistry Letters | Year: 2012

On the basis of scaffold hopping, a novel series of 2-alkyl-1- arylsulfonylprolinamides was discovered as 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) inhibitors. A representative compound 4ek, obtained through SAR and structure optimization studies, demonstrates excellent in vitro potency against 11β-HSD-1 and dose-dependent in vivo inhibition of 11β-HSD-1 in a prednisone/prednisolone transformation biomarker study in mice. © 2012 American Chemical Society.

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