A versatile approach to enantiopure (4S, 5R)-5-alkyl-4-hydroxy-2-pyrrolidinones is described. The key steps involve a regioselective Grignard reagent addition to (S)-malimides, and diastereoselective reductive dehydroxylation of the resulting hemi-azaketals. The flexibility of this methodology h...
Some novel 1-[2-[[5-(2-furanyl)-4-substituted 4H-1,2,4-triazol-3-yl]thio]ethyl]-2-methyl-5-nitro-1H-imidazoles (3), 1-[3-[[5-(2-furanyl/2-thienyl)-4-substituted 4H-1,2,4-triazol-3-yl]-thio]-2-hydroxypropyl]-2-methyl-5-nitro-1H-imidazoles (5) and 1-[3-[(N,N-disubstituted thiocarbamoyl)-thio]-2-hy...
Many natural and synthetic substances are known to interfere with the dynamic assembly of tubulin, preventing the formation of microtubules. In our search for potent and selective antitumor agents, a novel series of 1-(3′,4′,5′-trimethoxybenzoyl)-5-amino-1,2,4-triazoles were synthesized. The ...
In the present study, we report the discovery of a novel class of substituted 4-amino-2-thiopyrimidines as antiangiogenic and antiproliferative agents. Structural hybridization between 4-substituted aminopyrimidines (VEGFR-2 inhibitors) and 2-thioxopyrimidines (BRAF inhibitors) was carried out t...
Knowledge of the profile of fatty acids, including the profile of long chain fatty acids, is an important parameter for many areas like human health, food sciences, and the study of gene expression in plant tissues, among others. Moreover, very long chain fatty acids occur at low concentrations ...
A sensitive, selective and precise liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for determination of propofol (PRO) in rat serum and hair has been developed. 3-Bromomethyl-propyphenazone was used as derivatization reagent forming propofol-methyl-propyphenazone compound. The d...
Nerve agent metabolites (NAMs) derived from alkyl methyl phosphonic acids, such as ethyl methylphosphonic acid (EMPA), isopropyl methylphosphonic acid (IMPA), and pinacolyl methylphosphonic acid (PMPA), were extracted from human urine using diethyl ether as an extractant. After exchanging the di...
The synthesis and electrochromic properties of a novel regiosymmetric polymer based on 3,4-ethylenedioxythiophene, poly(2,3-bis(bromomethyl)-2,3-dihydrothieno[3,4-b][1,4]dioxine) (PEDOT(MeBr)2) were highlighted. The monomer was electrochemically polymerized via repetitive cycling between 0 and 1...
Non- and dinitro 4-bromomethyl-7-methyl coumarins and new mono- and trinitro 4-bromomethyl-7-methyl coumarins have been synthesized. Effect of nitro groups on the photophysical properties of the parent 4-bromomethyl-7-methyl coumarin has been reported. Their ground and excited state dipole momen...
The estrogenic effect of dietary 4-tert-octylphenol (octylphenol) in rainbow trout Oncorhynchus mykiss was investigated. Octylphenol was administered orally to sexually immature rainbow trout every second day for 11 days in doses between 0.4 and 50 mg kg−1 2 d−1. Plasma vitellogenin was measured...
The estrogenic effect of dietary 4-tert-octylphenol in the flounder Platichthys flesus was investigated in the laboratory. In the first experiment male flounders were fed doses of 10, 50 and 100 mg 4-tert-octylphenol kg−1 BW or 0.05 mg 17β-estradiol kg−1 BW every second day for 10 days. Increas...
Two bis-bromo substituted imidazo-[1,5-a]-pyridine derivatives IMPY1 and IMPY2 were synthesized from a 2:1:2 mixture of ortho/meta-bromobenzaldehyde, 2-cyanopyridine and ammonium acetate. The compounds IMPY1 and IMPY2 exhibit blue fluorescence in both THF and methanol solution and their highly f...
The structure of 3-(4-bromophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbaldehyde was determined by using X-ray diffraction analysis. Photophysical studies of the title compound were investigated in the solvents with different polarities. The emission spectrum of the compound was recorded in po...
A one-pot domino reaction involving Lewis acid-mediated nucleophilic-substitution/intramolecular-cyclization/reverse Claisen condensation of 2-(aryl(piperidin-1-yl)methyl)phenols and 1,3-diketones has been developed for the synthesis of 2-(3-oxo-1-phenylbutyl)phenyl acetates in good to excellent...
ObjectiveTo evaluate the treatment effects of the IL-6R antibody tocilizumab and cyclophosphamide (CTX) in patients with Takayasu arteritis (TA) and explore the mechanism by analyzing their effects on various cytokines.
Currently, process intensification research is focused on use of the continuous micro reactor over the batch reactors. The micro reactor process gives continuous product output, effective micro mixing and better yield in small residence time over batch reactors. A continuous flow process has bee...
This article describes the design of biphenyl moiety linked with aryl piperazine and syntheses of fourteen 1-(biphenyl-4-yl)-2-[4-(substituted phenyl)-piperazin-1-yl]ethanone derivatives along with their pharmacological evaluation for antipsychotic activity and computational studies including qu...
Cyclometalated Ir(III) complexes are widely used as phosphorescent materials in organic light-emitting diodes. In this work, the vibrationally resolved phosphorescence spectra of an experimental reported and four novel designed Ir(III) complexes with 2-(2,5,2′,3′,4′,5′,6′-heptafluoro-biphen...
We report herein the use of ferric iron (Fe3+) and sulfite (SO32−) to activate persulfate (S2O82−). Decolorization and mineralization of reactive Brilliant Red X-3B (a model azo dye) by an Fe(III)/sulfite/persulfate triple system have been investigated in aqueous solutions. Initial pH and dissol...
The facile syntheses of 1,2- and 3,5-cyclic sulfite and sulfate furanoside diesters were conducted in molecular solvents and ionic liquids in the presence of immobilised morpholine. Molecular solvents and ionic liquids performed similarly with regards to overall yields. However, the use of ILs a...
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