In the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by m...

The synthesis, structural characterization and in vitro biological evaluation of two 2-(4′-aminophenyl)benzothiazole based ligands and their corresponding Pd(II) and Pt(II) complexes is reported. Their design was based on the selective anticancer action of phenylbenzothiazole in conjunction wit...

A new series of biologically active Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) complexes derived from the novel thiosemicarbazone ligand; (E)-N′-(1-(4-aminophenyl)ethylidene)morpholine-4-carbothiohydrazide (HL) were synthesized. The mode of bonding of the ligand and the geometrical structures of...

With the aid of computer simulation, we have designed four covalent-organic frameworks based on tetrakis(4-aminophenyl)silsesquioxane (taps-COFs) and their hydrogen storage properties were predicted with grand canonical Monte Carlo (GCMC) simulation. The structural parameters and physical proper...

A novel dimeric gadolinium(III) complex, bis(4-Gd-DTPA-aminophenyl)adamantane (5), was successfully synthesized using bis(4-aminophenyl)adamantane to link two Gd-DTPA units. All the intermediates and bis(4-Gd-DTPA-aminophenyl)adamantane (5) have been characterized by 1H NMR, 13C NMR, ES-API-MS, ...

In the present work poly[N-(4-[4-(aminophenyl)methylphenylmethacrylamide])] (PAMMAm) was synthesized and characterized by Fourier transform infrared (FTIR) spectroscopy, scanning electron microscope (SEM), elemental analysis and proton nuclear magnetic resonance (1H NMR). The synthesized materia...

Five substituted 2-aryl-4-hydroxy-5-(2′-aminophenyl)-1,3-thiazoles have been studied for their fluorescence properties under neutral and alkaline conditions in solutions of various organic solvents. From comparison with the analogous 2-aryl-4-hydroxy-5-(2′-hydroxyphenyl)-1,3-thiazoles it is cl...

Antagonists of peripheral type 1 cannabinoid receptors (CB1) may have utility in the treatment of obesity, liver disease, metabolic syndrome and dyslipidemias. We have targeted analogues of the purine inverse agonist otenabant (1) for this purpose. The non-tissue selective CB1 antagonist rimonab...

The structure and thermal and photochemical decomposition of the synthetic precursor 5-chloro-3-trifluoromethyl-1,2,4-thiadiazole (1) have been investigated for the first time by mid-infrared, Raman, ultraviolet and He I photoelectron spectroscopy. Spectroscopies, supported by quantum-chemical c...

The most stable, optimized structure of the 2-amino-3-chloro-5-trifluoromethyl pyridine (ACTP) molecule was predicted by the density functional theory calculations using the B3LYP method with cc-pVQZ basis set. Antitumor activity of the ACTP molecule was evaluated by molecular docking analysis. ...

The preparation of (S)-3-methylamino-3-[(R)-pyrrolidin-3-yl]propanenitrile (1), a key fragment of fluoroquinolone antibiotic PF-00951966 and others was achieved by N-methylative aziridine ring opening, addition of methyl group at the ring nitrogen, and ring-opening via a cyanide nucleophile in a...

A combination of an amino-acid derived chiral phosphine catalyst and methyl acrylate has been employed to catalyze the direct Mannich reaction of α-aryl isocyanoacetate and N-Boc-aldimines efficiently. The loading of the catalyst could be as low as 0.5 mol% without compromise on the yield and e...

The polymerization by ATRP of hydroxy and amino functional acrylates and methacrylates with tert-butyldimethylsilyl (TBDMS) or tert-butyloxycarbonyl (BOC) protective groups has been studied for the first time achieving high control over molecular weight and polydispersity. Detailed investigation...

A highly enantioselective construction of an all-carbon quaternary stereogenic center at the α-position of malonic diesters has been achieved by Michael addition using phase-transfer catalysis. The reaction of α-monosubstituted malonates with acrylates in the presence of N-(9-anthracenylmethyl...

The fundamental possibility of acylative kinetic resolution of racemic heterocyclic amines was demonstrated by the example of all-cis-5-(4-bromophenyl)-4-tert-butoxycarbonyl-2-methoxycarbonylpyrrolidine. Individual enantiomers (ee >99%) were obtained in high yields via preparative chiral HPLC.

A range of 4-substituted derivatives of the pan class I PI 3-kinase inhibitor 2-(difluoromethyl)-1-[4,6-di-(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474) were prepared in a search for more soluble analogs. 4-Aminoalkoxy substituents provided the most potent derivatives, with the ...

The Cu(II) complex compound (Cu(C11H17N3O3)2Cl2(H2O)2) was synthesized from reaction between the copper(II) chloride dihydrate and the 4-ethoxy-2-methyl-5-(4-morpholinyl)-3(2H)-pyridazinone. The Cu(II) complex compound in octahedral geometry was characterized using elementel analysis, FT-IR and ...

The synthesis and characterization of a novel compound (S)-N-benzyl-1-phenyl-5-(pyridin-2-yl)-pent-4-yn-2-amine (abbreviated as BPPPYA) was presented in this study. The spectroscopic properties of the compound were investigated by FT-IR, NMR and UV spectroscopy experimentally and theoretically. ...

The synthesis of one pyrethroid insecticide [2-methyl-4-oxo-3-prop-2-yn-1-ylcyclopent-2-en-1-yl-3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate (Abbrev. JZ) (Fig. 1)] conjugated with a series of α-terthienyl derivatives (2–8) (Fig. 1) by palladium/copper-catalyzed cross-coupling reac...

The synthesis and in vitro evaluation of novel triazole-linked chloroquinoline derivatives as potential antiplasmodial agents against Plasmodium falciparum is reported. The 15 synthesized target compounds were obtained by means of a copper(I)-mediated click reaction between a variety of 1,2- and...