Synthesis of thyrotropin-releasing hormone analogs. 1. Complete dissociation of central nervous system effects from thyrotropin-releasing activity

…, L Kisfaludy, E Palosi, L Szporny

Index: Szirtes, Tamas; Kisfaludy, Lajos; Palosi, Eva; Szporny, Laszlo Journal of Medicinal Chemistry, 1984 , vol. 27, # 6 p. 741 - 745

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Citation Number: 60

Abstract

Twenty-four thyrotropin-releasing hormone (TRH) analogues containing mainly aliphatic amino acids in position 2 were synthesized and tested for central nervous system (CNS) and hormonal (TSH) activity. Application of the pentafluorophenyl ester method in the syntheses resulted in optimal yields and high purity of the products. The neutral tripeptides pGlu-Nva- Pro-NH2 (9), pGlu-Nle-Pro-NH2 (lo), and pGlu-Leu-Pro-NHp (3) with a three-or four- ...