[Alkyl derivatives of isoquinoline. III. Synthesis and pharmacologic activity of dialkylaminoalkyl amides of 1-chloro- and 1-methoxy-3-carboxy-4-methylisoquinoline and of 3-carboxy-2,4-dimethyl-1,2-dihydro-1-oxoisoquinoline].
The synthesis of a series of dialkylaminoalkylic amides of 1-chloro-3-carboxy-4-methylisoquinoline (VIII), of 1-methoxy-3-carboxy-4-methylisoquinoline (VI) and of 3-carboxy-2,4-dimethyl-1-oxoisoquinoline (XIII) is described. In addition a series of 1-amino-substituted 3-carboxymethyl-4-methylisoquinolines (II) was synthesized. The pharmacological activity of some of these compounds was studied. The compounds (XIIIa), (VIa) and (VIIIa) showed a clear local anaesthetic activity, a little lower than that of lidocaine; the same compounds also showed fairly good antispasmodic properties.
D000779:Anesthetics, Local / Q000138:chemical synthesis*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis; D001522:Behavior, Animal / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D005122:Exudates and Transudates / Q000187:drug effects; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000138:chemical synthesis*; D008297:Male; D051379:Mice; D010276:Parasympatholytics / Q000138:chemical synthesis*; D051381:Rats; D011919:Rats, Inbred Strains
D000779:Anesthetics, Local; D000893:Anti-Inflammatory Agents; D007546:Isoquinolines; D010276:Parasympatholytics
Ricerche su derivati alchilici della isochinolina. Nota III. Sintesi ed attività farmacologica di dialchilamminoalchilammidi della 1-cloro- e 1-metossi-3-carbossi-4-metilisochinolina e della 3-carbossi-2,4-dimetil-1,2-diidro-1-ossiisochinolina.