Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
The synthesis of (2RS)-1-(5-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and (2RS)-1-(7-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and its enantiomers, analogs of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol ((RS)-9) is described. Compounds were tested for electrographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for alpha(1)-, alpha(2)- and beta(1)-adrenoceptors binding affinities. The antagonist potency of the new compounds was compared with carvedilol and (RS)-9.
Groszek
Grazyna
G
Faculty of Chemistry, Rzeszów University of Technology, 6 Powstańców Warszawy Avenue, 35-959 Rzeszów, Poland. ggroszek@prz.edu.pl
Nowak-Król
Agnieszka
A
Wdowik
Tomasz
T
Swierczyński
Dariusz
D
Bednarski
Marek
M
Otto
Monika
M
Walczak
Maria
M
Filipek
Barbara
B
D019840:2-Propanol / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018674:Adrenergic Antagonists / Q000138:chemical synthesis* / Q000737:chemistry; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002227:Carbazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000077261:Carvedilol; D007082:Ileum / Q000187:drug effects; D008297:Male; D015394:Molecular Structure; D011412:Propanolamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013237:Stereoisomerism
D018674:Adrenergic Antagonists; D000959:Antihypertensive Agents; D002227:Carbazoles; D011412:Propanolamines; D000077261:Carvedilol; D019840:2-Propanol