Quantitative structure-activity relationships for N-[(N', N'-disubstituted-amino) acetyl] arylamines for local anesthetic activity and acute toxicity

F Heymans, L Le Therizien, JJ Godfroid…

Index: Heymans; Le Therizien; Godfroid; Bessin Journal of Medicinal Chemistry, 1980 , vol. 23, # 2 p. 184 - 193

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Citation Number: 12

Abstract

The synthesis and physicochemical properties of a series of N-[(N', N'-disubstituted-amino) acetyl] arylamines are described. A QSAR method is applied to local anesthetic activity and acute toxicity by means of a" nonclassic" substituent variation involving a modification on both aryl and amino moieties. The choice of the different parameters (partition coefficient, pK,, connectivity index, molar refraction, and molar volume) is discussed and their different ...