The role of the 4''-hydroxyl on motilin agonist potency in the 9-dihydroerythromycin series.

Article Details

Citation
Copy to clipboard

Liu Y, Carreras CW, Claypool M, Myles DC, Shaw SJ

The role of the 4''-hydroxyl on motilin agonist potency in the 9-dihydroerythromycin series.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3712-4. doi: 10.1016/j.bmcl.2011.04.078. Epub 2011 Apr 24.

PubMed ID
21570844 [ View in PubMed
]
Abstract

The role of the erythromycin 4''-hydroxyl group has been explored on the motilin agonist potential in the 9-dihydroerythromycin series of motilides. The compounds show potencies 2- to 4-fold superior to the corresponding hydroxylated compounds. The relationship is maintained when the 9-hydroxyl is alkylated to generate the corresponding 4''-deoxy-9-O-acetamido-9-dihydroerythromycins. However, concomitant with this increase in potency is an increase in hERG inhibition.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ErythromycinMotilin receptorEC 50 (nM)1000N/AN/ADetails