Počet záznamů: 1

Synthesis and biological activity of oxytocin analogues containing unnatural amino acids in position 9: structure activity study

  1. 1.
    0342937 - UOCHB-X 2011 RIV AT eng J - Článek v odborném periodiku
    Magafa, V. - Borovičková, Lenka - Slaninová, Jiřina - Cordopatis, P.
    Synthesis and biological activity of oxytocin analogues containing unnatural amino acids in position 9: structure activity study.
    Amino Acids. Roč. 38, č. 5 (2010), s. 1549-1559 ISSN 0939-4451
    Výzkumný záměr: CEZ:AV0Z40550506
    Klíčová slova: oxytocin antagonists * position 9 * unnatural amino acids * biological activity
    Kód oboru RIV: CC - Organická chemie
    Impakt faktor: 4.106, rok: 2010

    The paper reports the solid phase synthesis and pharmacological properties of 24 oxytocin analogues. Basic modifications at position 9 (L- nebo D-beta-(2-thienyl)-alanine, L- or D-3-Pyridylalanine) were combined with D-tyrosine(OEthyl) or D-1-naphthylalanine in position 2 and beta-mercaptopropionic acid in position 1. Additional 8 analogues had alpha-aminoisobutyric acid or D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in position 9. The analogue having the highest anti-oxytocic activity was [Mpa(1), D: -Tyr(Et)(2), Deg(9)]OT (pA2= 8.68).
    Trvalý link: http://hdl.handle.net/11104/0185538