2, 4-Disubstituted oxazoles and thiazoles as latent pharmacophores for diacylhydrazine of SC-51089, a potent PGE 2 antagonist

…, S Tsymbalov, A Stapelfeld, MA Savage

Index: Hallinan; Hagen, Timothy J.; Tsymbalov, Sofya; Stapelfeld, Awilda; Savage, Michael A. Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 1 p. 1 - 6

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Citation Number: 30

Abstract

8-Chlorodibenz [b, f][1, 4] oxazepine-10 (11H)-carboxylic acid, 2-[1-oxo-3-(4-pyridinyl) propyl] hydrazide, monohydrochloride (1, SC-51089) is a functional PGE2 antagonist selective for the EP1 receptor subtype with antinociceptive activity. 1, 2 Analogues of SC- 51089, in which the diacylhydrazine moiety has been replaced with 2, 4-disubstituted- oxazoles and-thiazoles, are described.