Authors: M. Pokorná 1; J. Čižmárik 1; E. Sedlárová 1; E. Račanská 2 Authors‘ workplace: Katedra farmaceutickej chémie Farmaceutickej fakulty Univerzity Komenského, Bratislava 2 Katedra farmakológie a toxikológie Farmaceutickej fakulty Univerzity Komenského, Bratislava 1 Published in: Čes. slov. Farm., 1999; , 80-86 Category:
Within the framework of a systematic study of phenylcarbamic acid derivatives with local anaes-thetic effects, a series of 1-methyl-2-piperidinoethylesters of 2-, 3 - and 4-alkoxy(methoxy to decylo-xy)phenylcarbamic acids and an unsubstituted derivative, i.e. 1-methyl-2-piperidinoethylester ofphenylcarbamic acid, were prepared. In the prepared series of compounds, the mutual relationshipof the surface local anaesthetic activity and some physical and physico-chemical parameters (g, pKa,pH of turbidity, log P, p, RMr, log k’) was studied and quantified by the method of QSAR analysis.The steric constants L and B4, molar refraction (MR), valence indices of molecular connectivity ( 1 c v ),the number of carbons of the alkoxysubstituent (Cx) and molecular mass (Mr) were also correlated.The study has revealed that there exists a linear relation between the number of the carbons of thealkoxysubstituent (Cx), tabulated or calculated values (Mr, L, B4, MR, 1 c v ) and experimentallyobtained physico-chemical parameters (RMr, log P, p, log k’, pH of turbidity, pKa).
Key words: 1-methyl-2-piperidinoethylester of alkoxyphenylcarbamic acids – local anaestheticactivity – structure–activity relationship
Don‘t have an account? Create new account
Enter the email address that you registered with. We will send you instructions on how to set a new password.
