Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Article Details

Citation

Ding FX, Shen HC, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Wang J, Tong X, Holt TG, Chen Q, Waters MG, Hammond ML, Tata JR, Colletti SL

Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3372-5. doi: 10.1016/j.bmcl.2010.04.013. Epub 2010 Apr 11.

PubMed ID
20452209 [ View in PubMed
]
Abstract

A series of pyrazolyl propionyl cyclohexenamides were discovered as full agonists for the high affinity niacin receptor GPR109A. The structure-activity relationship (SAR) studies were aimed to improve activity on GPR109A, reduce Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 2C9 (CYP2C9) inhibition, reduce serum shift and improve pharmacokinetic (PK) profiles.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
NiacinHydroxycarboxylic acid receptor 2EC 50 (nM)1000N/AN/ADetails
NiacinHydroxycarboxylic acid receptor 2IC 50 (nM)140N/AN/ADetails