Chalcone-based carbamates for Alzheimer's disease treatment

Future Medicinal Chemistry
Angela RampaAlessandra Bisi

Abstract

Alzheimer's disease is a still untreatable multifaceted pathology, and drugs able to stop or reverse its progression are urgently needed. In this picture, the recent reformulation of the cholinergic hypothesis renewed the interest for acetylcholinesterase inhibitors. In this paper, a series of naturally inspired chalcone-based carbamates was designed to target cholinesterase enzymes and possibly generate fragments endowed with neuroprotective activity in situ. Results & methodology: All compounds presented in this study showed nanomolar potency for cholinesterase inhibition. Notably, fragment 11d also displayed an interesting neuroprotective profile. These new derivatives are able to simultaneously modulate different key targets involved in Alzheimer's disease, and could be regarded as promising starting points for the development of disease-modifying drug candidates. [Formula: see text].

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Citations

May 16, 2017·Future Medicinal Chemistry·Maria Laura Bolognesi
Jul 25, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Matheus de Freitas SilvaAndrea Tarozzi
Aug 1, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Angela RampaAlessandra Bisi
Jul 3, 2019·Journal of Molecular Modeling·Vitor S DuarteHamilton B Napolitano
Sep 21, 2019·Mini Reviews in Medicinal Chemistry·Yaghoub PourshojaeiAli Asadipour
Jul 16, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Matheus de Freitas SilvaClaudio Viegas
Feb 12, 2021·Bioorganic Chemistry·Pritam ThapaMukut Sharma
Jul 15, 2020·ACS Chemical Neuroscience·Rita Maria Concetta Di MartinoFederica Belluti

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Methods Mentioned

BETA
column chromatography

Software Mentioned

dinger Suite
Glide
ChemDraw Professional
Schr Suite
Protein Preparation Wizard
Schr
LigPrep Suite

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