The phenylcarbamic acid derivatives with N-phenylpiperazine moiety in the molecule have been prepared. The structure has been confirmed by elemental analysis, IR, 1H NMR, and mass spectral data. For the prepared set of the compounds the lipophilicity parameters have been determined. The experimentally obtained lipophilicity parameters have been correlated with theoretical entries obtained by different computer programs based on the neural network and fragmental methods.
3-and 4-alkyloxyphenylcarbamoyloxy)-2-hydroxypropyl]piperazinium Chlorides. -A variety of title piperazine derivatives (IV) (11 examples) are synthesized and evaluated for their antiarrhythmic activity. Except for derivative (IVc), the most potent compound, all the compounds synthesized possess only moderate antiarrhythmic activity. -(MALIK, I.; SEDLAROVA, E.; CSOELLEI, J.; RACANSKA, E.; CIZMARIK, J.; KURFUERST, P.; Sci. Pharm. 72 (2004) 4, 283-291; Dep. Pharm. Chem., Fac. Pharm., Comenius Univ., SK-832 32 Bratislava, Slovakia; Eng.) -C. Hettrich
The basic physicochemical properties, lipophilicity parameters of dibasic alkyloxy-substituted phenylcarbamic acids were estimated. For the prepared set of compounds the experimentally obtained solubility, acidity, and lipophilicity parameters were correlated with those computed using various computer programs based on the associative artificial neural network and fragmental methods. The results of pharmacological evaluation were used as entry data for the complex correlations.
1-(4-fluoropheny1)-4-[3-(2-,3- and 4-alkyloxyphenylcarbamoyloxy)-2-hydroxypropyl]piperaziniumchlorides, with one to four carbon atoms in the alkoxy group on aromatic ring have been synthesized as the derivatives of substituted phenylcarbamic acid. The structures were confirmed by their spectral data. Potential antiarrhythmic activity was evaluated in guinea-pigs model. Preliminary studies demonstrated that the evaluated compounds, using ouabain arrhythmia model, appear to possess only moderate antiarrhythmic activity. Only compound marked as 4f appears to be more potent and lead us to focus our attention on structures with more bulky substituent in the m-position at aromatic ring in the hydrophilic part of molecule.
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