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 - 1992

Fingerprint

Adrenergic Receptors
Antihypertensive Agents
Potassium Channels
Derivatives
Clinical Studies

Keywords

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

ASJC Scopus subject areas

  • Molecular Medicine
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

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

In: European Journal of Medicinal Chemistry, Vol. 27, No. 2, 1992, p. 107-114.

Research output: Contribution to journalArticle

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, vol. 27, no. 2, pp. 107-114. https://doi.org/10.1016/0223-5234(92)90098-L
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. / Synthesis, antihypertensive and α-adrenoceptor activity of novel 2-aminoalkyl-3(2H)-pyridazinones. In: European Journal of Medicinal Chemistry. 1992 ; Vol. 27, No. 2. pp. 107-114.
@article{11a2ebbfa09f401ab506b83a3a5fdba7,
title = "Synthesis, antihypertensive and α-adrenoceptor activity of novel 2-aminoalkyl-3(2H)-pyridazinones",
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.",
keywords = "2-phenoxyalkylaminoalkyl-, 2-[1,4]benzodioxanylmethylaminoalkyl-3(2H)-pyridazinones, antihypertensive, α-adrenoceptor blocking activity",
author = "P. M{\'a}tyus and J. Kos{\'a}ry and E. Kasztreiner and N. Makk and E. Diesler and K. Czak{\'o} and G. Rabloczky and L. Jaszlits and E. Horv{\'a}th and Z. T{\"o}m{\"o}sk{\"o}zi and G. Cseh and E. Horv{\'a}th and P. Ar{\'a}nyi",
year = "1992",
doi = "10.1016/0223-5234(92)90098-L",
language = "English",
volume = "27",
pages = "107--114",
journal = "European Journal of Medicinal Chemistry",
issn = "0223-5234",
publisher = "Elsevier Masson SAS",
number = "2",

}

TY - JOUR

T1 - Synthesis, antihypertensive and α-adrenoceptor activity of novel 2-aminoalkyl-3(2H)-pyridazinones

AU - Mátyus, P.

AU - Kosáry, J.

AU - Kasztreiner, E.

AU - Makk, N.

AU - Diesler, E.

AU - Czakó, K.

AU - Rabloczky, G.

AU - Jaszlits, L.

AU - Horváth, E.

AU - Tömösközi, Z.

AU - Cseh, G.

AU - Horváth, E.

AU - Arányi, P.

PY - 1992

Y1 - 1992

N2 - 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.

AB - 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.

KW - 2-phenoxyalkylaminoalkyl-, 2-[1,4]benzodioxanylmethylaminoalkyl-3(2H)-pyridazinones

KW - antihypertensive, α-adrenoceptor blocking activity

UR - http://www.scopus.com/inward/record.url?scp=0026588242&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0026588242&partnerID=8YFLogxK

U2 - 10.1016/0223-5234(92)90098-L

DO - 10.1016/0223-5234(92)90098-L

M3 - Article

VL - 27

SP - 107

EP - 114

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

SN - 0223-5234

IS - 2

ER -