Referenced in: none

Automatically associated channels: Kv11.1

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

Authors: Yaoquan Liu, Yong Li, David C Myles, Mark Claypool, Christopher W Carreras, Simon J Shaw

Journal, date & volume: Bioorg. Med. Chem., 2010 Nov 1 , 18, 7651-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20869254

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.