Stúdium lokálnych anestetík. VXII. Príprava a úcinnost' dibázických alkylesterov 2-, a 3-alkoxy substituovaných kyselín fenylkarbámových
[Local anesthetics. VXII. Preparation and effectiveness of dibasic alkylesters of 2-, and 3-alkoxy-substituted phenylcarbamic acids]
Language Slovak Country Czech Republic Media print
Document type English Abstract, Journal Article
PubMed
8402965
- MeSH
- Anesthetics, Local * chemistry toxicity MeSH
- Carbamates * chemistry toxicity MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Animals MeSH
- Publication type
- English Abstract MeSH
- Journal Article MeSH
- Names of Substances
- Anesthetics, Local * MeSH
- Carbamates * MeSH
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.
Dibasic Derivatives of Phenylcarbamic Acid against Mycobacterial Strains: Old Drugs and New Tricks?