[Synthesis and pharmacologic activity of 3-quinolizidine-1'-yl-5-R-indoles].
By acid action on the mixture of homolupinal diethylacetal and arylhydrazines several 3-quinolizidin-1'-yl-5-R-indoles (III a - III e) were prepared. The homolupinal diethylacetal, whose hydrolysis gives rise to the unknown aldehyde, was obtained through the action of lupinylmagnesium chloride on diethylphenylorthoformate. Compounds (III) were subjected to wide pharmacological screening; all of them exhibited calcium blocking, negative cardioinotropic and diuretic activities, while single compounds showed antiinflammatory (III d), anticonvulsant and hypoglycemic (III e) activities.
Boido-Canu
C
C
Istituto di Scienze Farmaceutiche, Universita di Genova.
Boido
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V
Sparatore
F
F
Sparatore
A
A
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis; D000927:Anticonvulsants / Q000138:chemical synthesis; D002121:Calcium Channel Blockers / Q000138:chemical synthesis; D002316:Cardiotonic Agents / Q000138:chemical synthesis; D055598:Chemical Phenomena; D002621:Chemistry; D004232:Diuretics / Q000138:chemical synthesis; D006168:Guinea Pigs; D007004:Hypoglycemic Agents / Q000138:chemical synthesis; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D011807:Quinolizines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000927:Anticonvulsants; D002121:Calcium Channel Blockers; D002316:Cardiotonic Agents; D004232:Diuretics; D007004:Hypoglycemic Agents; D007211:Indoles; D011807:Quinolizines
Sintesi ed attività farmacologica di 3-chinolizidin-1'-il-5-R-indoli.