Development of a highly selective EP2-receptor agonist. Part 1: identification of 16-hydroxy-17,17-trimethylene PGE2 derivatives.

Abstract:

:Design and synthesis of an EP2-receptor selective agonist began with the chemical modification of alpha- and omega-chains of butaprost 1a, which exhibits an affinity for the IP-receptor. Two series of prostaglandin (PG) analogues with a 16-hydroxy-17,17-trimethylene moiety as an omega-chain were identified. Among those tested, 4a,b,e,f,h and 6a,b,e,f,h were found to be highly selective EP2-receptor agonists. Structure-activity relationships are discussed.

journal_name

Bioorg Med Chem

authors

Tani K,Naganawa A,Ishida A,Sagawa K,Harada H,Ogawa M,Maruyama T,Ohuchida S,Nakai H,Kondo K,Toda M

doi

10.1016/s0968-0896(01)00369-8

subject

Has Abstract

pub_date

2002-04-01 00:00:00

pages

1093-106

issue

4

eissn

0968-0896

issn

1464-3391

pii

S0968089601003698

journal_volume

10

pub_type

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