Synthesis and evaluation of novel pyrazolidinone analogs of PGE 2 as EP 2 and EP 4 receptors agonists

…, Y Liao, S Karra, N Brugger, D Fischer, E Palmer

Index: Zhao, Zhong; Araldi, Gian Luca; Xiao, Yufang; Reddy, Adulla P.; Liao, Yihua; Karra, Srinivasa; Brugger, Nadia; Fischer, David; Palmer, Elizabeth Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 23 p. 6572 - 6575

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Citation Number: 13

Abstract

Replacement of the hydroxy cyclopentanone ring in PGE2 with chemically more stable heterocyclic rings and substitution of the unsaturated α-alkenyl chain with a metabolically more stable phenethyl chain led to the development of potent and selective analogs of PGE2. Compound 10f showed the highest potency and selectivity for EP4 the receptor.