Antiamnesic properties of analogs and mimetics of the tripeptide human urocortin 3

G. Telegdy, Anita Kármen Kovács, Kinga Rákosi, Márta Zarándi, G. Tóth

Research output: Contribution to journalArticle

Abstract

Amnesia is a deficit in memory caused by brain damage, disease, or trauma. Until now, there are no successful medications on the drug market available to treat amnesia. Short analogs and mimetics of human urocortin 3 (Ucn 3) tripeptide were synthetized and tested for their action against amnesia induced by eletroconvulsion in mice. Among the 16 investigated derivatives of Ucn 3 tripeptide, eight compounds displayed antiamnesic effect. Our results proved that the configuration of chiral center of glutamine does not affect the antiamnesic properties. Alkyl amide or isoleucyl amide at the C-terminus may lead to antiamnesic compounds. As concerned the N-terminus, acetyl, Boc, and alkyl ureido moieties were found among the active analogs, but the free amino function at the N-terminus usually led to an inactive derivatives. These observations may lead to the design and synthesis of small peptidomimetics and amino acid derivatives as antiamnesic drug candidates, although the elucidation of the mechanism of the action requires further investigations.

Original languageEnglish
Pages (from-to)2261-2266
Number of pages6
JournalAmino Acids
Volume48
Issue number9
DOIs
Publication statusPublished - Sep 1 2016

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Keywords

  • Antiamnesic effect
  • Passive avoidance learning
  • Peptidomimetics
  • Urocortin 3 fragments

ASJC Scopus subject areas

  • Biochemistry
  • Clinical Biochemistry
  • Organic Chemistry

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