title: Synthesis and Pharmacological Activity of a New Series of 1-(1H-Indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol Analogs.
abstract: β-Adrenergic receptor antagonists are important therapeutics for the treatment of cardiovascular disorders. In the group of β-blockers, much attention is being paid to the third-generation drugs that possess important ancillary properties besides inhibiting β-adrenoceptors. Vasodilating activity of these drugs is produced through different mechanisms, such as nitric oxide (NO) release, β2 -agonistic action, α1 -blockade, antioxidant action, and Ca(2+) entry blockade. Here, a study on evaluation of the cardiovascular activity of five new compounds is presented. Compound 3a is a methyl and four of the tested compounds (3b-e) are dimethoxy derivatives of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol. The obtained results confirmed that the methyl and dimethoxy derivatives of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and their enantiomers possess α1 - and β1 -adrenolytic activities and that the antiarrhythmic and hypotensive effects of the tested compounds are related to their adrenolytic properties.
authors: Faculty of Pharmacy, Department of Pharmacological Screening, Medical College, Jagiellonian University, Krakow, Poland.
authors: Marek
authors: M
authors: Bednarski
authors: Faculty of Pharmacy, Department of Pharmacological Screening, Medical College, Jagiellonian University, Krakow, Poland.
authors: Monika
authors: M
authors: Otto
authors: Faculty of Pharmacy, Department of Pharmacological Screening, Medical College, Jagiellonian University, Krakow, Poland.
authors: Magdalena
authors: M
authors: Dudek
authors: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Medical College, Jagiellonian University, Krakow, Poland.
authors: Marcin
authors: M
authors: Kołaczkowski
authors: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Medical College, Jagiellonian University, Krakow, Poland.
authors: Adam
authors: A
authors: Bucki
authors: Faculty of Pharmacy, Department of Pharmacobiology, Medical College, Jagiellonian University, Krakow, Poland.
authors: Agata
authors: A
authors: Siwek
authors: Faculty of Chemistry, Rzeszów University of Technology, Rzeszów, Poland.
authors: Grażyna
authors: G
authors: Groszek
authors: Institute of Organic Chemistry, Warszawa, Poland.
authors: Elżbieta
authors: E
authors: Maziarz
authors: Nencki Institute of Experimental Biology, Warszawa, Poland.
authors: Piotr
authors: P
authors: Wilk
authors: Faculty of Pharmacy, Department of Pharmacological Screening, Medical College, Jagiellonian University, Krakow, Poland.
authors: Jacek
authors: J
authors: Sapa
mesh_terms: D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000959:Antihypertensive Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D005021:Ethylamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008958:Models, Molecular; D020005:Propanols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D018340:Receptors, Adrenergic, alpha-1 / Q000737:chemistry / Q000378:metabolism; D018342:Receptors, Adrenergic, beta-1 / Q000737:chemistry / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014665:Vasodilator Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000889:Anti-Arrhythmia Agents; D000959:Antihypertensive Agents; D005021:Ethylamines; D007211:Indoles; D020005:Propanols; D018340:Receptors, Adrenergic, alpha-1; D018342:Receptors, Adrenergic, beta-1; D014665:Vasodilator Agents
keywords: Cardiovascular activity; Enantiomers; Synthesis; α1-, α2-, β1-Adrenoreceptor antagonists