Synthesis and Pharmacological Activity of a New Series of 1-(1H-Indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol Analogs

被引:6
|
作者
Bednarski, Marek [1 ]
Otto, Monika [1 ]
Dudek, Magdalena [1 ]
Kolaczkowski, Marcin [2 ]
Bucki, Adam [2 ]
Siwek, Agata [3 ]
Groszek, Grazyna [4 ]
Maziarz, Elzbieta [5 ]
Wilk, Piotr [6 ]
Sapa, Jacek [1 ]
机构
[1] Jagiellonian Univ, Coll Med, Dept Pharmacol Screening, Fac Pharm, PL-30688 Krakow, Poland
[2] Jagiellonian Univ, Coll Med, Dept Pharmaceut Chem, Fac Pharm, PL-30688 Krakow, Poland
[3] Jagiellonian Univ, Coll Med, Dept Pharmacobiol, Fac Pharm, PL-30688 Krakow, Poland
[4] Rzeszow Univ Technol, Fac Chem, Rzeszow, Poland
[5] Inst Organ Chem, Warsaw, Poland
[6] M Nencki Inst Expt Biol, PL-02093 Warsaw, Poland
关键词
alpha(1)-; alpha(2)-; beta(1)-Adrenoreceptor antagonists; Cardiovascular activity; Enantiomers; Synthesis; PSYCHOLOGICAL SYMPTOMS; CARVEDILOL BLOCKS; BETA-BLOCKERS; DERIVATIVES; RECEPTOR; BUCINDOLOL; CURRENTS; PROTEIN;
D O I
10.1002/ardp.201500234
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
beta-Adrenergic receptor antagonists are important therapeutics for the treatment of cardiovascular disorders. In the group of beta-blockers, much attention is being paid to the third-generation drugs that possess important ancillary properties besides inhibiting beta-adrenoceptors. Vasodilating activity of these drugs is produced through different mechanisms, such as nitric oxide (NO) release, beta(2)-agonistic action, alpha(1)-blockade, antioxidant action, and Ca2+ 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 alpha(1)- and beta(1)-adrenolytic activities and that the antiarrhythmic and hypotensive effects of the tested compounds are related to their adrenolytic properties.
引用
收藏
页码:211 / 223
页数:13
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