Propranolol analogs containing natural monoterpene structures: synthesis and pharmacological properties.
A few derivatives of natural, bicyclic monoterpenes, which are propranolol analogs, were synthetized. Those compounds were studied pharmacologically in order to determine their toxicity, antiarrhythmic activity in selected experimental models of arrhythmia, the local anesthetic effect and influence on the cardiovascular system. The tested compounds showed a less potent or similar toxicity towards reference drugs, were devoid of an antiarrhythmic activity in the model of barium arrhythmia, yet some of them (compounds 9 and 12) increased the arrhythmogenic dose of strophanthin. All the compounds studied had a local anesthetic effect stronger than lidocaine in infiltration anesthesia, and compound 8--also in surface anesthesia.
Siemieniuk
A
A
Institute of Organic and Physical Chemistry, Polytechnical University, Wrocław, Poland.
Szałkowska-Pagowska
H
H
Lochyński
S
S
Piatkowski
K
K
Filipek
B
B
Krupińska
J
J
Czarnecki
R
R
Librowski
T
T
Białas
S
S
D000779:Anesthetics, Local; D000818:Animals; D001145:Arrhythmias, Cardiac / Q000517:prevention & control*; D001794:Blood Pressure / Q000187:drug effects*; D002849:Chromatography, Gas; D002855:Chromatography, Thin Layer; D005260:Female; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects*; D008297:Male; D051379:Mice; D011433:Propranolol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013729:Terpenes / Q000032:analysis
D000779:Anesthetics, Local; D013729:Terpenes; D011433:Propranolol