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Development of Novel API-ILs for the Optimization of Anti-Alzheimer Drugs

Departamento de Química Orgánica and Instituto de Investigación Sanitaria Galicia Sur (IISGS), Universidade de Vigo, 36310 Vigo, Spain
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Presented at the 22nd International Electronic Conference on Synthetic Organic Chemistry, 15 November– 15 December 2018; Available Online: https://sciforum.net/conference/ecsoc-22.
Proceedings 2019, 9(1), 47; https://doi.org/10.3390/ecsoc-22-05669
Published: 14 November 2018
PDF [260 KB, uploaded 19 April 2019]

Abstract

The current treatment of Alzheimer’s disease (AD) is mainly focused on enhancing the cholinergic neurotransmission by means of acetylcholinesterase inhibitors (AChEIs). Therefore, there is a growing interest in the development of novel AChEIs. New drugs should not only be able to inhibit the enzyme but also to show optimal parameters of solubility and permeability, since they affect drug bioavailability. Considering the potential advantages of transforming active pharmaceutical ingredients (APIs) into ionic liquids (ILs), five API-ILs derived from two AChEIs, tacrine and a donepezil analogue, were synthesized. The water solubility of these novel API-ILs was analyzed.
Keywords: ionic liquids; active pharmaceutical ingredients; acetylcholinesterase inhibitors; phthalazinone scaffold; water solubility ionic liquids; active pharmaceutical ingredients; acetylcholinesterase inhibitors; phthalazinone scaffold; water solubility
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Tornero, B.; Fernández-Stefanuto, V.; Tojo, E.; Besada, P.; Terán, C. Development of Novel API-ILs for the Optimization of Anti-Alzheimer Drugs. Proceedings 2019, 9, 47.

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