The objective of this study is to develop a novel in situ optical sensor for monitoring pesticides in water. The sensor consists of a polymer-coated attenuated total reflection (ATR) element or a silver halide optical fibre. The polymer film, which consists of PVC with a chloroparaffin plasticis...
The diffusion of a chloroparaffin from PE into benzene, chloroform, carbon tetrachloride and dioctyl phthalate has been studied at different temperatures and on sorption of benzene and dioctyl phthalate by the polymer. The diffusion coefficient of a chloroparaffin depends on the nature of the so...
The convenient synthesis of new aminomethylphosphinic acids and their derivatives containing N-alkyl 4-hydroxypiperidines moieties was developed. The addition of bis(trimethylsiloxy)phosphine to N-alkyl 4-piperidones proceeds under mild conditions to give PH-phosphinates as key compounds for pre...
The two-coordinate compound Zn{Si(SiHMe2)3}2 (1) is generated by the reaction of ZnCl2 and 2 equiv. of KSi(SiHMe2)3, but this species undergoes reductive elimination to produce (Me2HSi)3Si–Si(SiHMe2)3 and metallic zinc over 48 h at room temperature. The transient disilylzinc compound is stabili...
Progress in the subject of peptides and amino acids has enabled us to think beyond the standard 20 proteinogenic amino acids, the majority of which belong to a certain class of peptide secondary metabolites known as nonribosomal peptides (NRPs). The discovery of amino acids like pyrrolysine, sel...
A series of (1H-1,2,3-triazol-4-yl)methoxybenzaldehyde derivatives containing an anthraquinone moiety were synthesized and identified as novel xanthine oxidase inhibitors. Among them, the most promising compounds 1h and 1k were obtained with IC50 values of 0.6 μM and 0.8 μM, respectively, whic...
Aurora kinases play critical roles in the regulation of the cell cycle and mitotic spindle assembly. Aurora A kinase, a member of the Aurora protein family, is frequently highly expressed in tumors, and selective Aurora A inhibition serves as a significant component of anticancer therapy. Howeve...
Thioureas are exceptionally versatile building blocks towards the synthesis of wide variety of heterocyclic systems, which also possess extensive range of pharmacological activities. The substituted benzoic acids were converted into corresponding acid chlorides, these acid chlorides were then tr...
A target-free and cell-based approach was applied to evaluate the anti-influenza properties of six newly synthesized benzoic acid derivatives. SA-2, the ethyl 4-(2-hydroxymethyl-5-oxopyrrolidin-1-yl)-3-[3-(3-methylbenzoyl)-thioureido] benzoate (compound 2) was screened as a potential drug candid...
African trypanosomiasis is a neglected parasitic disease that is still of great public health relevance, and a severe impediment to agriculture in endemic areas. The pathogens possess certain unique metabolic features that can be exploited for the development of new drugs. Notably, they rely on ...
The synthesis of two enantiomeric pairs of pyrimidoisoindoles 9a, 9b and 10a, 10b is reported. During a domino ring-closure reaction, followed by cycloreversion, the chirality of diendo-(−)-(1R,2S,3R,4S)-3-aminobicyclo[2.2.1]hept-5-ene-2-carboxamide [(−)-1] was successfully transfered to heteroc...
We have discovered a potent low molecular weight series of HIV-1 Protease inhibitors incorporating the (R)-(hydroxyethyl) sulfonamide isostere.
In continuance with earlier reported work, an extension has been carried out by the same research group. Mulling over the ongoing condition of resistance to existing antimalarial agents, we had reported synthesis and antimalarial activity of certain pyrazole-1,3,4-oxadiazole hybrid compounds. Be...
A formal [4+1] annulation of readily available α-arylhydrazonoketones and dimethyl sulfonium methylides is described, which involving tandem ylide-mediated addition and nucleophilic cyclization reactions. This transformation features mild reaction conditions, simple execution, good to high yiel...
The 27Al, 15N, 13C and 1H NMR spectra in DMSO and mass spectra of 2:1 aluminium(III) complexes (1b–4b) derived from anthranilic acid azo coupling products with 4-tert.butylphenol (1a), 2-naphthol (2a) acetoacetanilide (3a) 3-methyl-1-phenylpyrazol-5-one (4a) were measured and analysed. It was f...
Fruitbodies of the mushroom Hebeloma sacchariolens reduce anthranilic acid (1a) and some of its analogues to the corresponding aromatic aminoaldehydes with high efficiency.
We report the preparation and characterization by elemental analysis, infrared (IR), single crystal X-ray diffraction, magnetic measurements and electron paramagnetic resonance (EPR) of the new compound catena-poly[copper(II)-μ-dichloro-l-lysine]hemihydrate, with formula C6H14Cl2CuN2O2·(H2O)0....
Publisher SummaryThis chapter discusses the assay procedure, purification, and properties of the S-adenosylmethionine: ɛ-N-lysine methyltransferase. The initial extract for the assay is prepared from Neurospora crassa 33933. The methyllysine transferase assay measures the formation of radioactiv...
In this work, green synthesis of a kind of fluorescent core-shell nanoparticles via a facile one-pot method was reported. We chose tryptophan, a common amino acid, to serve as the green reducing agent of the gold core. And a biomacromolecule, poly-(l-lysine), was then employed to assemble and cr...
To develop a multifunctional polymeric carrier for gene and drug co-delivery, a new cyclodextrin derivative containing poly(L-lysine) dendrons was prepared by the click conjugation of per-6-azido-β-cyclodextrin with propargyl focal point poly(L-lysine) dendron of third generation and then chara...
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