[Local anesthetics. VXII. Preparation and effectiveness of dibasic alkylesters of 2-, and 3-alkoxy-substituted phenylcarbamic acids].
In a series of 24 compounds of the type of dibasic alkylesters of 2-, and 3-alkoxy substituted phenylcarbamic acids, esterified alcohols 1-dipropylamino-3-pyrrolidino (piperidino or perhydroazepino)-2-propanol were used. It follows from the results of pharmacological evaluation that these compounds possess a high index of effectiveness in surface and infiltration anaesthesia compared to the standards of cocaine and procaine. Maximum effectiveness in surface anaesthesia was shown by [1-dipropylaminomethyl)-2- (piperidino)ethyl]-ester of 3-butoxyphenylcarbamic acids whose activity is as much as 180 times higher than that of cocaine. Maximum effectiveness in infiltration anaesthesia was shown by [1-dipropylaminomethyl)-2-(pyrrolidino)ethyl] ester of pentyloxyphenylcarbamic acid achieving an activity 250 times higher than that of standard procaine. The prepared compounds are more effective in the case of infiltration than in the case of surface anaesthesia.
Csöllei
J
J
Katedra farmaceutickej chémie Farmaceutickej fakulty Univerzity Komenského, Bratislava.
Búciová
L
L
Cizmárik
J
J
Kopácová
L
L
D000779:Anesthetics, Local / Q000737:chemistry / Q000633:toxicity; D000818:Animals; D002219:Carbamates / Q000737:chemistry / Q000633:toxicity; D013329:Structure-Activity Relationship
D000779:Anesthetics, Local; D002219:Carbamates