Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors.

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Bianchi DA, Hirschmann GS, Theoduloz C, Bracca AB, Kaufman TS

Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors.

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2711-5.

PubMed ID

15878275 [ View in PubMed

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Abstract

The synthesis of simplified analogs of the novel isoquinoline alkaloid stephaoxocanidine, carrying the oxazaphenalene ABC-ring system of the natural product, and their activity as inhibitors of the enzyme acetylcholinesterase, are reported. 5,6-Dimethoxy-7H -8-oxa-1-aza-phenalen-9-one (5) was as active as a Narcissus extract enriched in galantamine.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Tubocurarine	Acetylcholinesterase	Protein	Humans	Unknown	Inhibitor	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Physostigmine	Acetylcholinesterase	IC 50 (nM)	30	N/A	N/A	Details
Tacrine	Acetylcholinesterase	IC 50 (nM)	200	N/A	N/A	Details