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.
- 2-phenoxyalkylaminoalkyl-, 2-[1,4]benzodioxanylmethylaminoalkyl-3(2H)-pyridazinones
- antihypertensive, α-adrenoceptor blocking activity
ASJC Scopus subject areas
- Drug Discovery
- Organic Chemistry