Synthesis, Antiacetylcholinesterase Activity, and Molecular Dynamics Simulation of Aporphine–benzylpyridinium Conjugates
Nisachon Khunnawutmanotham,
Pichjira Sooknual,
Paratchata Batsomboon
et al.
Abstract:A series of aporphines conjugated with an Nbenzylpyridinium moiety through an amide-bond linkage were synthesized and evaluated for their acetylcholinesterase (AChE) inhibitory activity. The conjugation of the N-benzylpyridinium group significantly enhanced the AChE inhibitory activity of the core aporphine. The halogen substituents on the benzyl group affected the activity of the conjugates. Both (S)-and (R)enantiomers of three conjugates with low IC 50 values were synthesized and evaluated for their activiti… Show more
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