9-Dihydroerythromycin ethers as motilin agonists--developing structure-activity relationships for potency and safety.

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

9-Dihydroerythromycin ethers as motilin agonists--developing structure-activity relationships for potency and safety.

Bioorg Med Chem. 2010 Nov 1;18(21):7651-8. doi: 10.1016/j.bmc.2010.08.035. Epub 2010 Aug 19.

PubMed ID
20869254 [ View in PubMed
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Abstract

A series of derivatives of the amine of 9-dihydro-9-O-ethylamino-N-desmethyl-N-isopropyl erythromycin A derivatives were synthesized as motilin agonists. The compounds were developed for potency without showing antibacterial activity and inhibition of the hERG potassium channel. The formamide of the amide series was found to show the optimal combination of properties relative to carbamates, ureas, thioureas, and amines. This prompted an investigation of heterocyclic isosteres for the amide. In this series the triazole had the optimal combination of properties. From the study, two compounds met the criteria for detailed pharmacokinetic studies.

DrugBank Data that Cites this Article

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