A series of 2-(5-(6-Bromo-2-methyl-4-oxoquinazolin-3(4H)-yl)-4H-1,2,4-triazole-3-ylthio)-N-(substituted benzylidene) acetohydrazides (5a-5l) have been synthesized via condensation of 2-(5-(6-Bromo-2-methyl-4-oxaquinazolin-3 (4H)-yl)-4H-1,2,4-triazole-3-ylthio)acetohydrazide (4) with different aromatic aldehydes. Cycloaddition of thioglycolic acid with 5a-5l yielded 2-[5-(6-Bromo-2-methyl-4-oxoq...

A series of (1H-benzo[d][1,2,3]triazol-1-yl)(4-benzylpiperazin-1-yl)methanones and of (1H-benzo[d][1,2,3]triazol-1-yl)(4-phenylpiperazin-1-yl)methanones has been prepared and tested on human fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). In the benzylpiperazinyl series, compound 29 (ML30) exhibited an IC(50) value of 0.54 nM on MAGL, combined with a 1000-fold selectivity ...

Two hexanuclear rhenium clusters containing azide ligands, [Re6Se8(PEt3)5(N3)]BF4 and [Re6Se8(PEt3)4(N3)2], were synthesized from the analogous pyridine complexes and fully characterized. Studies show that [Re6Se8(PEt3)5(N3)]BF4 reacts with activated alkynes, dimethyl acetylenedicarboxylate and methyl 4-hydroxyhex-2-yneoate, to form the triazolate cluster complexes [Re6Se8(PEt3)5(L1 or L2)]BF4 ...

UNLABELLED Current SPECT radioligands available for in vivo imaging of the dopamine transporter (DAT) also show affinity for monoamine transporters other than DAT, especially the serotonin transporter (SERT). The effect of this lack of selectivity for in vivo imaging is unknown. In this study, we compared the SPECT radioligands (123)I-2-β-carbomethoxy-3β-(4-iodophenyl)-N-(3-fluoropropyl)nortrop...

Matrix metalloproteinase 2 (MMP-2) contains three fibronectin type II (col) modules that contribute to its collagen specificity. We observed that the CD spectra of the separate col modules account for the CD and temperature profiles of the in-tandem col-123 construct. Thus, to the extent of not significantly perturbing the secondary structure and thermal stability characteristics of the neighbo...

In this study, the effects of solvents and molecular structure upon acidity, five 3-alkyl(aryl)-4-phthalimido-4,5-dihydro-1H-1,2,4-triazol-5-ones (3-7) were potentiometrically titrated with tetrabutylammonium hydroxide (TBAH) in four different anhydrous (isopropyl alcohol, acetonitrile, tert-butyl alcohol N,N-dimethylformamide) HNP corresponding pKa values determined by half-neutralization meth...