Le Douaron, Gael’s team published research in Journal of Medicinal Chemistry in 2016-07-14 | 89898-96-4

Journal of Medicinal Chemistry published new progress about Alkynylation. 89898-96-4 belongs to class quinoxaline, and the molecular formula is C8H5N3O3, Safety of 7-Nitro-2(1H)-quinoxalinone.

Le Douaron, Gael; Ferrie, Laurent; Sepulveda-Diaz, Julia E.; Amar, Majid; Harfouche, Abha; Seon-Meniel, Blandine; Raisman-Vozari, Rita; Michel, Patrick P.; Figadere, Bruno published the artcile< New 6-Aminoquinoxaline Derivatives with Neuroprotective Effect on Dopaminergic Neurons in Cellular and Animal Parkinson Disease Models>, Safety of 7-Nitro-2(1H)-quinoxalinone, the main research area is aminoquinoxaline preparation arylation alkynylation reaction neuroprotective effect dopamine neuron; Parkinson disease model neuroprotective effect dopamine aminoquinoxaline derivative.

Parkinson’s disease (PD) is a neurodegenerative disorder of aging characterized by motor symptoms that result from the loss of midbrain dopamine neurons and the disruption of dopamine-mediated neurotransmission. There is currently no curative treatment for this disorder. To discover druggable neuroprotective compounds for dopamine neurons, the authors have designed and synthesized a 2nd-generation of quinoxaline-derived mols. based on structure-activity relation studies, which led previously to the discovery of the authors’ 1st neuroprotective brain penetrant hit compound MPAQ (5c). Neuroprotection assessment in PD cellular models of the authors’ newly synthesized quinoxaline-derived compounds led to the selection of a better hit compound, PAQ (4c). Extensive in vitro characterization of 4c showed that its neuroprotective action is partially attributable to the activation of reticulum endoplasmic ryanodine receptor channels. Most interestingly, 4c was able to attenuate neurodegeneration in a mouse model of PD, making this compound an interesting drug candidate for the treatment of this disorder.

Journal of Medicinal Chemistry published new progress about Alkynylation. 89898-96-4 belongs to class quinoxaline, and the molecular formula is C8H5N3O3, Safety of 7-Nitro-2(1H)-quinoxalinone.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider