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

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 shape of molecules have a positive influence on their local anaesthetic activity, while contributions of aromatic CH and singly bonded nitrogen are negative. Since the estimated PASS probabilities to find local anaesthetic activity in the most active compounds are less than 50%, these compounds may be considered to be possible NCEs.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Geronikaki A,Vicini P,Dabarakis N,Lagunin A,Poroikov V,Dearden J,Modarresi H,Hewitt M,Theophilidis G

doi

10.1016/j.ejmech.2008.04.006

subject

Has Abstract

pub_date

2009-02-01 00:00:00

pages

473-81

issue

2

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(08)00207-9

journal_volume

44

pub_type

杂志文章

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