Synthesis, antihypertensive and α-adrenoceptor activity of novel 2-aminoalkyl-3(2H)-pyridazinones

P. Mátyus, J. Kosáry, E. Kasztreiner, N. Makk, E. Diesler, K. Czakó, G. Rabloczky, L. Jaszlits, E. Horváth, Z. Tömösközi, G. Cseh, E. Horváth, P. Arányi

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

A number of 2-phenoxyalkylaminoalkyl- and 2-[1,4]benzodioxanylmethylaminoalkyl-3(2H)-pyridazinones were synthesized and tested for hypotensive and antihypertensive activity as well as for α1- and α2-adrenoceptor binding affinities. Some derivatives, eg 5.5, 5.9, 5.12, 6.4 and 6.10, showed strong hypotensive/antihypertensive effect and high affinity for α2- and α1-adrenoceptors. Compound 5.5 was selected for clinical study. In its mode of action a potassium channel opening activity may also be involved.

Original languageEnglish
Pages (from-to)107-114
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume27
Issue number2
DOIs
Publication statusPublished - Mar 1992

Keywords

  • 2-phenoxyalkylaminoalkyl-, 2-[1,4]benzodioxanylmethylaminoalkyl-3(2H)-pyridazinones
  • antihypertensive, α-adrenoceptor blocking activity

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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  • Cite this

    Mátyus, P., Kosáry, J., Kasztreiner, E., Makk, N., Diesler, E., Czakó, K., Rabloczky, G., Jaszlits, L., Horváth, E., Tömösközi, Z., Cseh, G., Horváth, E., & Arányi, P. (1992). Synthesis, antihypertensive and α-adrenoceptor activity of novel 2-aminoalkyl-3(2H)-pyridazinones. European Journal of Medicinal Chemistry, 27(2), 107-114. https://doi.org/10.1016/0223-5234(92)90098-L