Synthesis of Angiotensin II Antagonists with Variations in Position 5

Olga Nyéki, Katalin Sz Szalay, Laios Kisfaludy, Egon Kárpáti, László Szporny, Gábor B. Makara, Bertalan Varga

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Six angiotensin II antagonists containing cyclohexylglycine (Chg) or cyclopentylglycine (Cpg) in position 5 were synthesized by stepwise elongation in solution, using the pentafluorophenyl ester method. The influence of substitution on the inhibitory properties of the analogues was studied in four different bioassays. [Sar1,Chg5,Lac8]AII proved to be the most potent antagonist with low intrinsic activity in both the in vitro and in vivo tests.

Original languageEnglish
Pages (from-to)1719-1724
Number of pages6
JournalJournal of Medicinal Chemistry
Volume30
Issue number10
DOIs
Publication statusPublished - Oct 1 1987

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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  • Cite this

    Nyéki, O., Szalay, K. S., Kisfaludy, L., Kárpáti, E., Szporny, L., Makara, G. B., & Varga, B. (1987). Synthesis of Angiotensin II Antagonists with Variations in Position 5. Journal of Medicinal Chemistry, 30(10), 1719-1724. https://doi.org/10.1021/jm00393a006