Design and synthesis of a highly selective EP4-receptor agonist. Part 1: 3,7-dithiaPG derivatives with high selectivity

T Maruyama; M Asada; T Shiraishi; A Ishida; H Egashira; H Yoshida; T Maruyama; S Ohuchida; H Nakai; K Kondo; M Toda

doi:10.1016/s0960-894x(01)00364-x

Design and synthesis of a highly selective EP4-receptor agonist. Part 1: 3,7-dithiaPG derivatives with high selectivity

Bioorg Med Chem Lett. 2001 Aug 6;11(15):2029-31. doi: 10.1016/s0960-894x(01)00364-x.

Authors

T Maruyama¹, M Asada, T Shiraishi, A Ishida, H Egashira, H Yoshida, T Maruyama, S Ohuchida, H Nakai, K Kondo, M Toda

Affiliation

¹ Minase Research Institute, Ono Pharmaceutical Co., Ltd., Shimamoto, Mishima, 618-8585, Osaka, Japan. to.maruyama@ono.co.jp

PMID: 11454473
DOI: 10.1016/s0960-894x(01)00364-x

Abstract

A series of 3,7-dithiaPGE(1) analogues 3, 4, 11, 16 and 19 were identified as highly selective EP4-receptor agonists starting from the chemical modification of 7-thiaPGE(1) analogue 1. EP4-receptor selectivity and agonist activity were maximized in 3 and 4.

MeSH terms

Alkenes / chemical synthesis*
Alkenes / pharmacology*
Animals
Binding Sites
CHO Cells / metabolism
Cricetinae
Cyclic AMP / agonists*
Cyclopentanes / chemical synthesis*
Cyclopentanes / pharmacology*
Drug Design
Humans
Ligands
Mice
Receptors, Prostaglandin E / agonists*
Receptors, Prostaglandin E, EP4 Subtype
Sensitivity and Specificity
Sulfur / chemistry*

Substances

Alkenes
Cyclopentanes
Ligands
PTGER4 protein, human
Ptger4 protein, mouse
Receptors, Prostaglandin E
Receptors, Prostaglandin E, EP4 Subtype
Sulfur
Cyclic AMP