Divergent structure–activity relationships of structurally similar acetylcholinesterase inhibitors

…, L Berg, C Engdahl, W Qian, F Ekström…

Index: Andersson, C. David; Forsgren, Nina; Akfur, Christine; Allgardsson, Anders; Berg, Lotta; Engdahl, Cecilia; Qian, Weixing; Ekstroem, Fredrik; Linusson, Anna Journal of Medicinal Chemistry, 2013 , vol. 56, # 19 p. 7615 - 7624

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Citation Number: 17

Abstract

The molecular interactions between the enzyme acetylcholinesterase (AChE) and two compound classes consisting of N-[2-(diethylamino) ethyl] benzenesulfonamides and N-[2- (diethylamino) ethyl] benzenemethanesulfonamides have been investigated using organic synthesis, enzymatic assays, X-ray crystallography, and thermodynamic profiling. The inhibitors' aromatic properties were varied to establish structure–activity relationships ( ...