Referenced in: none

Automatically associated channels: Kv11.1

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

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

Journal, date & volume: Bioorg. Med. Chem. Lett., 2011 Jun 15 , 21, 3712-4

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/21570844

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.