Shanghai Pharmaceutical Holding Co.

Ha’erlong, China

Shanghai Pharmaceutical Holding Co.

Ha’erlong, China
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Liu H.-Y.,Shanghai Pharmaceutical Holding Co.
Chinese Journal of Pharmacology and Toxicology | Year: 2013

In drug discovery and development, it is important to understand the routes of elimination, the contribution of each route to overall clearance and the enzymes involved in metabolism. The fraction of the dose cleared via cytochrome P450(CYP)-dependent metabolism (fm) in the liver can be evaluated using a human radiolabeled study, and the contribution of each CYP form to total CYP-mediated metabolism (fCYP) in the liver can be evaluated using in vitro phenotyping method. The product of fm and fCYP450 (fm x fCYP) is the contribution of CYP enzyme form to overall clearance, and it is one of the key determinants of the magnitude of drug-drug interactions. This paper reviewed different approaches to identification of the CYP form and determination of the contribution of each CYP form to total CYP-mediated metabolism.


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.


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.


PubMed | Shanghai Pharmaceutical Holding Co.
Type: Journal Article | Journal: Yao xue xue bao = Acta pharmaceutica Sinica | 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.

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