Evaluation of the local anaesthetic activity of 3-aminobenzo [d] isothiazole derivatives using the rat sciatic nerve model

…, N Dabarakis, A Lagunin, V Poroikov, J Dearden…

Index: Geronikaki, Athina; Vicini, Paola; Dabarakis, Nikos; Lagunin, Alexey; Poroikov, Vladimir; Dearden, John; Modarresi, Hassan; Hewitt, Mark; Theophilidis, George European Journal of Medicinal Chemistry, 2009 , vol. 44, # 2 p. 473 - 481

Full Text: HTML

Citation Number: 32

Abstract

On the basis of computer prediction of biological activity by PASS and toxicity by DEREK, the most promising 32-alkylaminoacyl derivatives of 3-aminobenzo [d] isothiazole were selected for possible local anaesthetic action. This action was evaluated using an in vitro preparation of the isolated sciatic nerve of the rat and compared with lidocaine which was used as a reference compound. QSAR studies showed that the polarizability, polarity and molecular ...