[Alkyl and aryl derivatives of isoquinoline. II. Synthesis and pharmacologic activity of dialkylaminoalkyl esters of 1-chloro-3-carboxy-4-methylisoquinoline and the corresponding 4-phenyl derivative].
The synthesis of a series of dialkylaminoalkylic esters of 1-chloro-3-carboxy-4-methylisoquinoline and of 1-chloro-3-carboxy-4-phenylisoquinoline is described. The pharmacological activity of some of these compounds was studied. The morpholinoethylester of 1-chloro-3-carboxy-4-methylisoquinoline (VIIa), dimethylaminoethylester (VIIb) and diethylaminoethylester (VIIc) showed a good antispasmodic activity. 4-Phenyl-derivatives (XVa), (XVb), (XVc) were more active than analogous 4-methyl derivatives; particularly the diethylaminoethylester of 1-chloro-3-carboxy-4-phenylisoquinoline (XVc) showed an antagonist effect against spasmogens similar to that of papaverine.
D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000700:Analgesics / Q000138:chemical synthesis; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis; D001464:Barium / Q000037:antagonists & inhibitors; D002490:Central Nervous System / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000138:chemical synthesis; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010276:Parasympatholytics / Q000138:chemical synthesis*; D051381:Rats; D011919:Rats, Inbred Strains
D000700:Analgesics; D000893:Anti-Inflammatory Agents; D006633:Histamine Antagonists; D007546:Isoquinolines; D010276:Parasympatholytics; D001464:Barium; D000109:Acetylcholine
Ricerche su derivati alchilici ed arilici della isochinolina. Nota II. Sintesi ed attività farmacologica di dialchilamminoalchilesteri della 1-cloro-3-carbossi-4-metilisochinolina e corrispondenti 4-fenilderivati.