A small set of 5-HT3 receptor ligands has been evaluated with regard to their potential AChE inhibitory activity with the aim of discovering new compounds interfering with acetylcholine release and degradation. The inhibitory activity has been theoretically rationalized in terms of the interaction with an AChE crystallographic model. Compounds 2 and 3 inhibited the enzyme at a concentration lower than 1.5 muM, while 6 established an interaction energy with AChE comparable to tacrine, but with insufficient conformational reorganization.
Alcaro, S., Ortuso, F., Battaglia, D., Anzini, M., Cappelli, A., Gallelli, A., et al. (2003). Enzymatic and Molecular Modeling Studies of 5-HT3 Receptor Ligands Based on Pyrroloquinoline Structure and Provided with Acetylcholinesterase Inhibitory Activity. MEDICINAL CHEMISTRY RESEARCH, 12(3), 147-160.
Enzymatic and Molecular Modeling Studies of 5-HT3 Receptor Ligands Based on Pyrroloquinoline Structure and Provided with Acetylcholinesterase Inhibitory Activity
Anzini, Maurizio;Cappelli, Andrea;Vomero, Salvatore;
2003-01-01
Abstract
A small set of 5-HT3 receptor ligands has been evaluated with regard to their potential AChE inhibitory activity with the aim of discovering new compounds interfering with acetylcholine release and degradation. The inhibitory activity has been theoretically rationalized in terms of the interaction with an AChE crystallographic model. Compounds 2 and 3 inhibited the enzyme at a concentration lower than 1.5 muM, while 6 established an interaction energy with AChE comparable to tacrine, but with insufficient conformational reorganization.
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https://hdl.handle.net/11365/9140
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