Journal of Medicinal Chemistry published new progress about 63598-71-0. 63598-71-0 belongs to triazoles, auxiliary class Triazole, name is 4H-1,2,4-Triazole, and the molecular formula is C2H3N3, Name: 4H-1,2,4-Triazole.
Fray, M. Jonathan published the artcileStructure-Activity Relationships of 1,4-Dihydro-(1H,4H)-quinoxaline-2,3-diones as N-Methyl-D-aspartate (Glycine Site) Receptor Antagonists. 1. Heterocyclic Substituted 5-Alkyl Derivatives, Name: 4H-1,2,4-Triazole, the publication is Journal of Medicinal Chemistry (2001), 44(12), 1951-1962, database is CAplus and MEDLINE.
A series of 6,7-dichloro-1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones were prepared in which the 5-position substituent was a heterocyclylmethyl or 1-(heterocyclyl)-1-Pr group. Structure-activity relationships were evaluated where binding affinity for the glycine site of the N-methyl-D-aspartate (NMDA) receptor was measured using the specific radioligand [3H]-L-689,560, and functional antagonism was demonstrated by inhibition of NMDA-induced depolarizations of rat cortical wedges. The ability to prevent NMDA-induced hyperlocomotion in mice in vivo was measured for selected compounds Binding affinity increased significantly if the heterocyclic group, e.g. 1,2,3-triazol-1-yl could participate in accepting a hydrogen bond from the receptor. It was difficult to obtain compounds with adequate aqueous solubility and strategies to improve it were investigated. The most potent compound in this series, 6,7-dichloro-5-[1-(1,2,4-triazol-4-yl)propyl]-1,4-dihydro-(1H,4H)-quinoxaline-2,3-dione (I) (binding IC50 = 2.6 nM; cortical wedge EC50 = 90 nM), inhibited NMDA-induced hyperlocomotion in mice (6/9 protected at 20 mg/kg iv). Pharmacokinetic parameters, including extent of brain penetration, for I and 6,7-dichloro-5-[(1-propyl-4-imidazolyl)methyl]-1,4-dihydro-(1H,4H)-quinoxaline-2,3-dione are reported.
Journal of Medicinal Chemistry published new progress about 63598-71-0. 63598-71-0 belongs to triazoles, auxiliary class Triazole, name is 4H-1,2,4-Triazole, and the molecular formula is C2H3N3, Name: 4H-1,2,4-Triazole.
Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics