Synthesis of thyrotropin-releasing hormone analogs. 2. Tripeptides structurally greatly different from TRH with high central nervous system activity

…, L Kisfaludy, E Palosi, L Szporny

Index: Szirtes, Tamas; Kisfaludy, Lajos; Palosi, Eva; Szporny, Laszlo Journal of Medicinal Chemistry, 1986 , vol. 29, # 9 p. 1654 - 1658

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Citation Number: 40

Abstract

A new series of thyrotropin-releasing hormone (TRH) analogues, obtained by further modifications of our most potent central nervous system (CNS) stimulating neutral tripeptides at both termini, were synthesized by the pentafluorophenyl ester method and tested for CNS and thyrotropin (TSH) releasing activity. Replacement of pyroglutamic acid by pyro-2- aminoadipic acid, 2-oxoimidazolidine-4-ca~ boxylic acid or y-butyrolactone-y-carboxylic ...