BECAS
BISCUSSI brunella
artículos
Título:
New Caffeine Derivatives as Multitarget Agents for the Therapy of Alzheimers Disease
Autor/es:
BISCUSSI, BRUNELLA; ANA PAULA MURRAY
Revista:
Chemistry Proceedings
Editorial:
MDPI
Referencias:
Lugar: Basel; Año: 2022 vol. 12 p. 1 - 5
ISSN:
2673-4583
Resumen:
Abstract: In this work we present the microwave-assisted synthesis and in vitro acetylcholinesteraseinhibition of a series of new caffeine derivatives. The design of these new compounds was inspiredby the caffeinepyrrolidine hybrids that act as AChE inhibitors and nAChR activators, previouslyreported by our group. All of the new caffeine analogs inhibited AChE. Among them, the compound2b (1,3-dimethyl-7-(6-(piperidin-1-yl)hexyl)-3,7-dihydro-1H-purine-2,6-dione) showed the strongesteffect (IC50 = 0.17 µM) on AChE, with higher potency than caffeinepyrrolidine hybrids. Thesepreliminary studies suggest that these new compounds might be interesting multifunctional drugsdestined to stimulate cholinergic signage.