9-Dihydroerythromycins as non-antibiotic motilin receptor agonists
Yaoquan Liu1, Yong Li, Yue Chen
1Department of Chemistry, Kosan Biosciences, Inc, 3832 Bay Center Place, Hayward, CA 94545, USA. gyliu@comcast.net
Abstract:
A series of 9-dihydroerythromycin A and B analogues with modification of the desosamine nitrogen have been synthesized and screened for motilin agonist activity, antibiotic activity, tachyphylaxis and hERG channel current inhibition. Small alkyl groups resulted in the potency while compounds with a primary or secondary amine resulted in the low motilin agonist potency. Several compounds were identified as non-antibiotic motilin receptor agonists with minimal tachyphylaxis and low hERG interaction.
Related Concept Videos
Drugs Affecting GI Tract Motility: Dopamine Receptor Antagonists
Drugs Affecting GI Tract Motility: Serotonin Receptor Agonists
Drugs Affecting GI Tract Motility: Opioids as Antidiarrheal Agents
Opioids, widely used antidiarrheal agents, mitigate diarrhea by slowing down...
Drugs Affecting GI Tract Motility: Antimicrobials as Antidiarrheal Agents
Antiasthma Drugs: Muscarinic Receptor Antagonists
Antimuscarinic agents compete with ACh for the same binding site on the muscarinic receptors. By binding to these receptors, they inhibit the downstream effects of ACh and block the parasympathetic...
Cholinergic Antagonists: Pharmacokinetics


