Substituted 2??benzothiazolamines as sodium flux inhibitors: Quantitative structure–activity relationships and anticonvulsant activity

…, DF Ortwine, G Johnson, RD Schwarz…

Index: Hays; Rice; Ortwine; Johnson; Schwarz; Boyd; Copeland; Vartanian; Boxer Journal of Pharmaceutical Sciences, 1994 , vol. 83, # 10 p. 1425 - 1432

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Citation Number: 110

Abstract

Abstract Thirty-two aryl-substituted 2-benzothiazolamines have been tested for their ability to modulate sodium flux in rat cortical slices. A QSAR analysis, applied to these derivatives, showed a trend toward increasing potency as sodium flux inhibitors with increasing lipophilicity, decreasing size, and increasing electron withdrawal of the benzo ring substitutents. Additionally, 4-or 5-substitution of the benzo ring was found to decrease ...