Synthesis of New Galanthamine-Peptide Derivatives Designed for Prevention and Treatment of Alzheimer's Disease

Current Alzheimer Research
Lyubomir T VezenkovNikolai Danchev

Abstract

Although no effective treatment for the Alzheimer's disease currently exist, some drugs acting as Acetylcholinesterase inhibitors, like galanthamine have positively affected such patients. β- and/or γ-secretase inhibitors are another type of potential drugs. Here we report synthesis of new peptide-galanthamine derivatives, with expected inhibitory activity against both Acetylcholinesterase and β-secretase. The aim of this work is obtaining new peptide derivatives of galanthamine with decreased toxicity compared to galanthamine. Syntheses were conducted in solution using fragment condensation approach. The new derivatives were characterized by melting points, angle of optical rotation, NMR and Mass spectra. Acute toxicity was determined on mice, according to a Standard protocol. All new compounds were tested in vitro for cytotoxic activity in a panel of human (HEP-G2, BV-173) and murine (Neuro-2a) tumor cell lines via a standard MTT-based colorimetric method. New derivatives of galanthamine containing shortened analogues of β-secretase inhibitor (Boc- Asn-Leu-Ala-Val-OH) and either nicotinic or isonicotinic residue, both connected with a linker (L-Asp) to position 11 of galanthamine were obtained. In vivo toxicity of some new co...Continue Reading

References

Oct 1, 1991·Trends in Pharmacological Sciences·J Hardy, D Allsop
Mar 4, 1994·Journal of Medicinal Chemistry·J L VidalucM Briley
Feb 24, 2001·Annals of the New York Academy of Sciences·P H St George-Hyslop
Mar 3, 2009·Journal of the Neurological Sciences·Balpreet MatharuBrian Austen
Jun 11, 2009·Protein and Peptide Letters·Lyubomir T VezenkovGalya I Ivanova

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Citations

Dec 4, 2020·Bulletin of Experimental Biology and Medicine·I I KostadinovaV V Rozhanets
Aug 24, 2021·Journal of Alzheimer's Disease : JAD·Maria I LazarovaReni E Kalfin

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