Synthesis and biological assessment of racemic benzochromenopyrimidinetriones as promising agents for Alzheimer's disease therapy

Future Medicinal Chemistry
Youssef DgachiLhassane Ismaili

Abstract

Due to the complex nature of Alzheimer's disease, there is a renewed search for multitarget directed drugs. This paper describes the synthesis and in vitro biological evaluation of six racemic 13-aryl-2,3,4,13-tetrahydro-1H,12H-benzo[6,7]chromeno[2,3-d]pyrido[1,2-a]pyrimidine-7,12,14-triones (1a-6a), and six racemic 15-aryl-8,9,10,11,12,15-hexahydro-14H-benzo[6',7']chromeno[2',3:4,5] pyr-imido [1,2-a]azepine-5,14,16-triones (1b-6b), showing antioxidant and cholinesterase inhibitory capacity. Among these compounds, 13-phenyl-2,3,4,13-tetrahydro-1H,12H-benzo[6,7]chromeno[2,3-d]pyrido[1,2-a]pyrimidine-7,12,14-trione (1a) is a nonhepatotoxic at 300 μmol/l dose concentration, and a selective EeAChE inhibitor showing good antioxidant power. A new family of racemic benzochromenopyrimidinetriones has been investigated for their potential use in the treatment of Alzheimer's disease.

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Citations

May 16, 2017·Future Medicinal Chemistry·Maria Laura Bolognesi
Sep 21, 2019·Mini Reviews in Medicinal Chemistry·Yaghoub PourshojaeiAli Asadipour
Aug 23, 2020·International Journal of Molecular Sciences·Todd J EckroatSeth C Cowan
Apr 15, 2021·ACS Chemical Neuroscience·Lukas GoreckiMaria Laura Bolognesi

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