62465-90-1Relevant academic research and scientific papers
Development of Radiolabeled Ligands Targeting the Glutamate Binding Site of the N-Methyl-d-aspartate Receptor as Potential Imaging Agents for Brain
Tamborini, Lucia,Chen, Ying,Foss, Catherine A.,Pinto, Andrea,Horti, Andrew G.,Traynelis, Stephen F.,De Micheli, Carlo,Mease, Ronnie C.,Hansen, Kasper B.,Conti, Paola,Pomper, Martin G.
, p. 11110 - 11119 (2016/12/30)
Abnormal activity of various N-methyl-d-aspartate receptor (NMDAR) subtypes has been implicated in a wide variety of neurological disorders such as Alzheimer's disease, schizophrenia, and epilepsy. Imaging agents for PET and SPECT that target NMDARs in a subtype-selective fashion may enable better characterization of those disorders and enhance drug development. On the basis of a pyrazoline derivative that demonstrated neuroprotective effects in vivo, we synthesized a series of para-substituted analogues and measured their affinities to various NMDAR subtypes. Compounds 4a-c and 4e showed greater, nanomolar affinity for the GluN1/2A subtype versus GluN1/2B. Dicarbomethoxy (pro-drug) analogues of [124/125I]4d and [11C]4e (i.e., [124/125I]11d and [11C]11e) were generated and tested for NMDAR binding specificity in ex vivo autoradiography and brain biodistribution studies. Although NMDAR-specific binding could be demonstrated for [125I]11d and [11C]11e through autoradiography and biodistribution studies, imaging of neither [124I]11d nor [11C]11e could demonstrate brain penetration sufficient for detection by PET.
HETEROCYCLES FROM NITRILE IMINES. PART I. 1,2,3,4-TETRAHYDRO-1,2,4,5-TETRAZINES
El-Abadelah, Mustafa M.,Hussein, Ahmad Q.,Kamal, Marwan R.,Al-Adhami, Khaled H.
, p. 917 - 924 (2007/10/02)
The interaction between ketohydrazones and nitrile imines provides a new and direct synthetic route to 1,2,3,4-tetrahydro-1,2,4,5-tetrazines.Elemental analysis and spectral data are consistent with the assigned tetrazine ring system.
COPPER(II) IN ORGANIC SYNTHESIS. VI REACTION OF THE COPPER(II) ACETATE COMPLEX OF 1-METHYLISATIN-3-CHLOROPHENYLHYDRAZONE WITH DIMETHYL ACETYLENEDICARBOXYLATE.
Coda, Corsico A.,Desimoni, G.,Invernizzi, Gamba A.,Quadrelli, P.,Righetti, P. P.,Tacconi, G.
, p. 2843 - 2852 (2007/10/02)
The copper(II) complex of 1-methylisatin -3-p-chlorophenylhydrazone (2) reacted with dimethyl acetylenedicarboxylate (DMAD) in accordance to two reaction pathways.Oxidation performed by Cu(2+) gave 1-metyl-3-carbenindolin-2-one (12), trapped by DMAD to gi
Synthesis of New 2,5-Dihydro-1,2,3,5-Thiatriazole 1-Oxides and 3,4-Dihydro-2H-1,2,4,3-triazaphosphole 3-Oxides
Heubach, Guenther
, p. 1376 - 1383 (2007/10/02)
Methyl 2-alkylamino- or 2-arylamino-2-(2-arylhydrazono)acetates 1 react with thionyl chloride in the absence of bases to give 5-alkyl- or 5-aryl-4-methoxycarbonyl-2,5-dihydro-1,2,3,5-thiatriazole 1-oxides 3.Reaction of alkylphosphonic dichlorides and 2 mo
