A high-throughput (HTS) and high-content screening (HCS) campaign of a commercial library identified 2,3-dihydroimidazo[1,2-a]benzimidazole analogues as a novel class of anti-parasitic agents. A series of synthetic derivatives were evaluated for their in vitro anti-leishmanial and anti-trypanoso...
A synthetic small molecule, 1-[(1H-indol-3-yl)methylene]-2-phenylhydrazine (HMPH) was conveniently synthesised by a one-step reaction, purified and characterised by chromatographic and spectroscopic methods. HMPH scavenged free radicals and inhibited lipopolysaccharide (LPS)-induced ROS generati...
Selective targeting of cancer cells over normal cells is a key objective of targeted therapy. However few approaches achieve true mechanistic selectivity resulting in debilitating side effects and dose limitation. In this work we describe the discovery of A131 (4a), a new agent with an unprecede...
The syntheses, characterizations and structures of three novel dichloro(bis{2-[1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl-κN3]pyridine-κN})metal(II), [M(L)2Cl2], complexes (metal = Mn, Co and Ni) are presented. In the solid state the molecules are arranged in infinite hydrogen-bonded 3D supramo...
The present work deals with the green solar assisted synthesis of chalcone (3-(4-fluorophenyl)-1-(4-methoxyphenyl)-prop-2-en-1-one). To check the efficacy of the process, chalcone has been synthesized by photochemical (UV radiation), thermal method (60 °C) and the conventional method. The effec...
ObjectivesCrude extracts of Dodonaea viscosa var. angustifolia (DVA), has shown to have anticariogenic property. However the compound responsible for this activity has not been identified. The aim of this study was to investigate anti-acidogenic and anti-biofilm activity of a flavone 5,6,8-Trihy...
The synthesis of benzylacetone from benzyl alcohol and of 4-(4-methoxyphenyl)butan-2-one from 4-methoxybenzyl alcohol, which were previously performed in a batch cascade, were successfully performed in a telescoped flow system consisting of three micropacked bed reactors and a tube-in-tube membr...
A potential organic nonlinear optical (NLO) material 3-(4-dimethylamino)phenyl)1-(4-methoxyphenyl)prop-2-en-1-one (DMLNH2MC) with a molecular formula C18H19NO2 has been synthesized and crystallized in ethanol solution. The crystals of DMLNH2M were characterized using NMR and FTIR spectroscopy te...
A novel series of Schiff bases 4a–n was prepared from 2-hydrazinyl-N-(2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl) ethyl)acetamide. Thiazolidinone 5a–n derivatives were prepared from the reaction of Schiff base and thioglycolic acid. The structures of the synthesized compounds were assigned on ...
Carboxymethylcellulose (CMC) acts as a coating material for a magnesium-layered hydroxide-3-(4-methoxyphenyl)propionate (MLH-MPP) nanocomposite via spontaneous self-assembly. The resulting product is called a magnesium-layered hydroxide-3-(4-methoxyphenyl)propionate/carboxymethylcellulose (MLH-M...
Four new fluorescent dyes, composed of a 4-methoxyphenyl-pyridinium electron donor-acceptor pair, were synthesized and their solvatofluorochromism was investigated in thirteen different solvents with a wide range of polarities. Their different solvatofluorochromism behavior was rationalized by c...
Reversed-phase liquid chromatography coupled with electrospray ionization tandem mass spectrometry (ESI-MS/MS) was used to characterize impurities in cefpodoxime proxetil, an ester-modified prodrug. Based on the mechanisms by which cephalosporins are degraded, stress tests were designed and perf...
The inhibition of β secretase (BACE1) is potentially important approach to treatment of Alzheimer disease (AD). A novel series of 4-bromophenyl piperazine derivatives coupled to the phenylimino-2H-chromen-3-carboxamide scaffold were investigated as BACE1 inhibitors in this study. Docking study ...
Two novel bipolar Ir(III) complexes named (Czppy)2Ir(tfmptz) and (Czppy)2Ir(pptz) were synthesized and characterized, where the Czppy is 9-(4-(pyridin-2-yl)phenyl)-9H-carbazole, tfmptz refers to 2-(3-(trifluoromethyl)-1H-1,2,4-triazol-5-yl)pyridine and Hpptz represents 2-(1H-tetrazol-5-yl)pyridi...
One-pot solvothermal treatments of acetonitrile, water, LiOH, Cu(CH3COO)2·H2O and 3-(5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl)pyridine (HL) yielded a rare copper cyanide coordination polymer, [Cu2(L) (CN)]n (1). The existence of a cyanide group in compound 1 may be due to the decomposition of ace...
Treatment of 1-(2,5-dimethylphenyl)piperazine and 1-(2,3-dimethylphenyl)piperazine with H2SO4 in 2:1 molar ratio at RT affords the corresponding sulfate salts [C12H20N2][HSO4]2·H2O (SI) and [C12H20N2][HSO4]2 (SII). These compounds have been characterized by X-ray diffraction, thermal analysis a...
Uracil bearing a tethered allyl alcohol appendage at N1 undergoes a [2+2] photocycloaddition reaction to provide a single tricyclic adduct in high yield. This compound is transformed in one step into a cis-cyclobutane β-amino acid bearing a 3-hydroxymethyl group. Through appropriate functionali...
A series of waterborne polyurethane(WPU) dispersions containing different amounts of trimethylol propane(TMP) and/or 2-[(2-aminoethyl)amino]ethanesulfonic acid sodium salt (AAS salt), were synthesized by prepolymer emulsification process. The effects of TMP and AAS salt on properties of WPU disp...
Aqueous two-phase system (ATPS) containing salts has been used for protein purification and enrichment. However, it is unclear how proteins are partitioned in the top or bottom phases of the system. In this study, we demonstrate that the partition of proteins in salt-containing ATPS (SATPS) depe...
Michael addition of hetero-nucleophiles to active vinylogous imine intermediates generated in situ from 3-(1-arylsulfonylalkyl)-7-azaindoles has been described. This new strategy provides a facile and efficient approach to valuable 3-alkyl substituted 7-azaindole derivatives containing heteroato...
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