Within the constantly growing number of histamine H4 (H4R) receptor ligands there is a large group of azine derivatives. A series of novel compounds in the group of 4-methylpiperazine-1,3,5-triazine-2-amines were designed and obtained. Considered structures were modified at the triazine 6-positi...

Using a functional high-throughput screening (HTS) and subsequent SAR studies, we have discovered a novel series of non-nucleoside dengue viral polymerase inhibitors. We report the elaboration of SAR around hit compound 1 as well as the synthesis and antiviral evaluation of 3-phenyl-5-[(E)-2-(th...

The complexes Tb(L1)3·2H2O (I) {where L1 = 2′-hydroxy-4′-methoxy-2-phenylacetophenone}, Tb(L2)3·2H2O (II) {where L2 = 2′-hydroxy-4′-methoxy-2-(p-methoxyphenyl)acetophenone}, Tb(L3)3·2H2O (III) {where L3 = 2′-hydroxy-4′,6′-dimethoxy-2-phenylacetophenone} and Tb(L4)3·2H2O (III) {where L...

The complexes Eu(L1)3·2H2O (I) [where L1=2′-hydroxy-4′-methoxy-2-phenylacetophenone], Eu(L2)3·2H2O (II) [where L2=2′-hydroxy-4′-methoxy-2-(p-methoxyphenyl) acetophenone], Eu(L3)3·2H2O (III) [where L3=2′-hydroxy-4′, 6′-dimethoxy-2-phenylacetophenone] and Eu(L4)3·2H2O (IV) [where L4=2′...

A series of new quinazolinone based mono azo reactive dyes (D1–10) have been prepared by subsequent diazotization of 2-phenyl-3-[4′-(4″-aminophenylsulphonamido)]phenyl-4(3H)-quinazolinone-6-sulphonic acid (C) and coupling with various 4-chloro anilino cyanurated coupling components. These dye...

The photophysical properties and photochemistry reactions of 2-(2-Hydroxy-phenyl)-4(3H)-quinazolinone (HPQ) system in different solutions are studied by using density functional theory (DFT) and time-dependent density functional theory (TDDFT) methods. Our theoretical investigation explores that...

Pyrolysis of 5H-dibenzo[a,d]cyclohepten-5-one oxime (8) and 10,11-dihydro-5H-dibenzo-[a,d]cyclohepten-5-one oxime (9) in a flow system (at 1.33 mbar and 650°C) were examined comparatively with pyrolysis of benzophenone oxime (1a) using GC/MS. The pyrolysis products of 8 were: 1-cyanophenanthren...

[123I]-8-[4-[2-(5-Iodothienyl)]-4-oxobutyl]-3-methyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (1) (Ki D2 = 1.9 nM, Ki 5-HT2D2 = 16.7, log P7.5 = 3.14) has been synthesized as a selective ligand for dopamine D2 receptors. The in vivo distribution of the corresponding radioligand, 123I-1, was st...

Herein are studied new transformations of ethyl-4,4,4-trifluoroacetoacetate (ETFAA), giving access to a series of enantiopure chirons bearing both a trifluoromethyl group and an amino moiety. The key intermediate is obtained optically pure by a resolution procedure.

Optimization details and limitations of a novel synthetic method of 4-tert-butyl 2-ethyl 3-amino-1-benzyl-5-dialkylamino-1H-pyrrole-2,4-dicarboxylate derivatives are herein disclosed. This synthesis consists of four steps that include a highly selective cyclization, and can be carried out from s...

A family of dipeptidyl enoates has been prepared and tested against the parasitic cysteine proteases rhodesain, cruzain and falcipain-2 related to sleeping sickness, Chagas disease and malaria, respectively. They have also been tested against human cathepsins B and L1 for selectivity. Dipeptidyl...

The synthesis of α-benzylamino-β,γ-unsaturated acids has been developed starting from α-bromo-α,β-unsaturated chlorides. Via treatment of the acyl chlorides with (R)-pantolactone in the presence of TEA, the in situ formation of the deconjugated ketenes and their direct transformation into ...

The study of new dipolar A-π-D molecules, which have an acceptor (A) and donor (D) charge joined by a conjugate bridge, have been an attention focus in the recent years due their different properties. In the current work, a molecular system has been modified in order to compare the effect on pr...

A new macrocyclic hexanuclear manganese(III) 18-azametallacrown-6 compound, [Mn6(ashz)6(CH3OH)3(H2O)3] · 3H2O · 3DMF (1), has been prepared using a trianionic pentadentate ligand N-acetylsalicylhydrazide (ashz3−) and characterised by various techniques such as elemental analysis, IR, UV-vis an...

The crystal structure, spectroscopic properties and catalytic property of the copper(II) complex, prepared by the reaction between copper(II) diacetate with the bidentate Schiff base, SalAHE (SalAHE = salicylaldehydeimine-1-hydroxyethane), are reported. This complex is able to oxidize 3,5-di-ter...

The rates of autooxidation of 3,5-di-tert-butylcatechol and hydrolysis of p-nitrophenyl diphenyl phosphate in various mixed micelles formed from copper(II) surfactants and sodium dodecyl sulphate, cetyltrimethylammonium bromide and octaethylene glycol monododecyl ether were measured under the co...

The rates of the autooxidation of 3,5-di-tert-butylcatechol (3,5-DTBC) in transition metal ions (Cu2+, Co2+, Mn2+) in the presence of sodium dodecyl sulphate were investigated at 25°C in the acidic pH region. The results show that the maximum rate enhancement occurs at the cmc region.

Prussian Blue-modified iron oxide (PB-Fe2O3) nanoparticles (NPs) have been demonstrated to exhibit peroxidase-like activity through catalytic oxidation of the peroxidase substrate 3,5-di-tert-butylcatechol (3,5-DTBC) in the presence of H2O2, producing a yellow-colored solution. Kinetic analysis ...

The autoxidation of 3,5-di-tert-butylcatechol (H2DTBC) was catalyzed by the dicopper (II) complex, Cu2(dppn)(OH)Cl3·H2O (Cu2(dppn)(OH)3+). Kinetic studies determined that the reactants were first order in the concentrations of the catalytic dinuclear copper species, molecular oxygen, and H2DTBC...

The oxidation reaction of 3,5-di-tert-butylcatechol (dbcatH2) with dioxygen to 3,5-di-tert-butyl-o-benzoquinone (dbq) initiated by 2,2,6,6-tetramethyl-1-piperidinyloxyl (TEMPO) has been investigated in methanol and CCl4 at ambient temperature. The oxidation of dbcatH2 was followed by electron sp...