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Molecules

Title:		Deep Eutectic Solvents as Effective Reaction Media for the Synthesis of 2-Hydroxyphenylbenzimidazole-based Scaffolds en Route to Donepezil-Like Compounds
Author(s):		Piemontese L; Sergio R; Rinaldo F; Brunetti L; Perna FM; Santos MA; Capriati V;
Address:		"Dipartimento di Farmacia-Scienze del Farmaco, Universita degli Studi di Bari <>, Via E. Orabona 4, I-70125 Bari, Italy. Consorzio C.I.N.M.P.I.S., Via E. Orabona 4, I-70125 Bari, Italy. Centro de Quimica Estrutural, Instituto Superior Tecnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisboa, Portugal"
Journal Title:		Molecules
Year:		2020
Volume:		20200128
Issue:		3
Page Number:		-
DOI:		10.3390/molecules25030574
ISSN/ISBN:		1420-3049 (Electronic) 1420-3049 (Linking)
Abstract:		"An unsubstituted 2-hydroxyphenylbenzimidazole has recently been included as a scaffold in a series of hybrids (including the hit compound PZ1) based on the framework of the acetylcholinesterase (AChE) inhibitor Donepezil, which is a new promising multi-target ligand in Alzheimer's disease (AD) treatment. Building upon these findings, we have now designed and completed the whole synthesis of PZ1 in the so-called deep eutectic solvents (DESs), which have emerged as an unconventional class of bio-renewable reaction media in green synthesis. Under optimized reaction conditions, the preparation of a series of 2-hydroxyphenylbenzimidazole-based nuclei has also been perfected in DESs, and comparison with other routes which employ toxic and volatile organic solvents (VOCs) provided. The functionalization of the aromatic ring can have implications on some important biological properties of the described derivatives and will be the subject of future studies of structure-activity relationships (SARs)"
Keywords:		Benzimidazoles/*chemical synthesis/chemistry Donepezil/*chemistry Green Chemistry Technology Solvents/*chemical synthesis/chemistry Structure-Activity Relationship 2-hydroxyphenylbenzimidazole Alzheimer's disease deep eutectic solvents;
Notes:		"MedlinePiemontese, Luca Sergio, Roberta Rinaldo, Federica Brunetti, Leonardo Perna, Filippo M Santos, M Amelia Capriati, Vito eng 2017A5HXFC_002/Ministero dell'Istruzione, dell'Universita e della Ricerca/ Switzerland 2020/02/06 Molecules. 2020 Jan 28; 25(3):574. doi: 10.3390/molecules25030574"