Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists

Yufang Xiao; Gian Luca Araldi; Zhong Zhao; Nadia Brugger; Srinivasa Karra; David Fischer; Elizabeth Palmer

doi:10.1016/j.bmcl.2007.05.025

Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4323-7. doi: 10.1016/j.bmcl.2007.05.025. Epub 2007 May 16.

Authors

Yufang Xiao¹, Gian Luca Araldi, Zhong Zhao, Nadia Brugger, Srinivasa Karra, David Fischer, Elizabeth Palmer

Affiliation

¹ Department of Medicinal Chemistry, EMD Serono Research Institute, Inc., Rockland, MA 02370, USA. yufang.xiao@emdserono.com

PMID: 17531488
DOI: 10.1016/j.bmcl.2007.05.025

Abstract

Analogs of PGE(2) with introduction of diene groups at the omega-side chain have been synthesized and evaluated for their binding affinity for EP(2) and EP(4) receptors. An optimized analog (compound 9b) showed high potency and selectivity for the EP(4) receptor over other known receptors.

MeSH terms

Animals
Cell Line
Dinoprostone / analogs & derivatives*
Dinoprostone / pharmacokinetics
Dinoprostone / pharmacology
Half-Life
Humans
Rats
Receptors, Prostaglandin E / agonists*
Receptors, Prostaglandin E, EP2 Subtype
Receptors, Prostaglandin E, EP4 Subtype

Substances

PTGER2 protein, human
PTGER4 protein, human
Receptors, Prostaglandin E
Receptors, Prostaglandin E, EP2 Subtype
Receptors, Prostaglandin E, EP4 Subtype
Dinoprostone