Derivatives of 2-mercaptobenzenesulphonamide. XXI. Syntheses and cardiovascular effects of N-(dimethylaminoethyl)amides of 2-(perhydropyrimidin-2-yliminosulphonyl)-phenylthioalkanoic acids.
A series of 2-[5-chloro-4-methyl-2-(perhydropyrimidin-2-yl iminosulphonyl)phenylthio]alkanoic acids [IV-XI], their methyl esters [XII-XIX], N-(2-dimethylaminoethyl) amides, [XX-XXV] and the corresponding hydrochlorides [XXa-XXIVa] were obtained. The hydrochlorides [XXa, XXIIa, XXIVa] exhibited a comparable or stronger antiarrhythmic activity than the reference drugs, quinidine and procainamide. The influence of the tested compounds on the blood pressure and heart rate of rats as well as the acute toxicity in mice were studied. Some structure-activity relationship were also discussed.
Pomarnacka
E
E
Department of Chemical Drug Technology, Medical University of Gdańsk, Poland.
Oledzka
K
K
D000818:Animals; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000517:prevention & control; D002317:Cardiovascular Agents / Q000138:chemical synthesis*; D007928:Lethal Dose 50; D051379:Mice; D051381:Rats; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D002317:Cardiovascular Agents; D013438:Sulfhydryl Compounds; D013449:Sulfonamides