Traumatic brain injury affects a number of individuals per year and is a major cause of worldwide death and disability. Yet, its pathophysiological mechanism remains unclear. It is well-known that glial cells, including microglia and astrocytes, are activated and involved in tissue damage and re...

Controlled radical polymerization of methyl methacrylate and styrene initiated by azobisisobutironitrile or benzoyl peroxide in the presence of a chlorine-containing complex of FeIII with 5,15-bis(4’-tert-butylphenyl)-2,8,12,18-tetra(n-butyl)-3,7,13,17-tetramethylporphyrin was investigated.

The addition of organocerium reagents (from both organolithium and organomagnesium precursors) to chiral aldehyde hydrazones prepared from 1-aminoproline derivatives has been studied. The additions proceed in good yield and high diastereoselectivity and with good nucleophile (Me, n-Bu, i-Pr, t-B...

A DDE-degrading bacterium, Janibacter sp. TYM3221, is able to grow on biphenyl and degrades 1,1-dichloro-2,2-bis(4-chlorophenyl)ethylene (DDE) via a meta-ring cleavage pathway. The bphAa gene, encoding a biphenyl dioxygenase large subunit, was previously demonstrated to be involved in the degrad...

A series of chromone-2-carboxamido-alkylbenzylamines were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer’s disease (AD). The results showed that most of these compounds exhibited good multifunctional activities. Among them, compound 49 displayed exc...

Ir-catalysed alkylation of tert-butyl cyanoacetate with a range of substituted benzyl and heteroaryl alcohols under solvent free conditions afforded the corresponding monoalkylated products in moderate to high yields.

We report on methods of synthesis of new hexafluorobenzene- and decafluorobiphenyl-based hydroxyl-substituted phenyl ethers containing allyl, acetyl groups, and bromine atoms. Optimal conditions for Claisen and Fries rearrangements used during the synthesis of these fluorinated compounds are dis...

Functional aryl ethers bearing mono- and di-substituted azo compounds, allyl functionalities, vinyl phenyl moieties, trifluoromethyl (CF3) groups, etc. were prepared by nucleophilic substitution reaction of 2,3,4,5,6-pentafluorobenzonitrile (PFBN) in a stepwise manner at room temperature in dipo...

Due to the activation of fluorine atoms in aromatic rings by four other fluorine atoms and a 4-ethynyl bond, polyfluoroalkoxy chains can be introduced into aromatic rings by direct nucleophilic substitution reaction using potassium carbonate as base to prepare 4-polyfluoroalkoxy-2,3,5,6-tetraflu...

The pyrolyses of 4-phenyl-2,3,5,6-tetrafluorophenyl prop-2-enyl ether (26) under flash vapour phase (FVP) conditions at 350°C and of 4-trifluoromethyl-2,3,5,6-tetrafluorophenyl prop-2-enyl ether (27) on heating in vacuo at 169°C give mixtures of products which include 3-phenyl-2,4,5,7-tetraflu...

The titled compound (2) is prepared by oxidation of tris(4-amino-2,3,5,6-tetrafluorophenyl) methane with 98% H2O2 and trifluoroacetic anhydride. Compound 2, a strong carbon acid, forms long-persisting deep blue solutions of the anion on reaction with alkalis, amines, and alcohols. Oxidation of t...

The present communication deals with the synthesis of a series of 2-acetyl-2-ethoxycarbonyl-1-[4(4′-arylazo)-phenyl]-N,N-dimethylaminophenyl aziridines. The compounds were synthesized in excellent yields (70–80%) and the structures were established on the basis of consistent IR, 1H NMR and ele...

6-N-Hydroxylaminopurine (HAP) prolonged the survival time of mice bearing sarcoma 180 ascites cells; several other ascitic neoplasms were less sensitive to this agent. The rate of incorporation of 2-14C-glycine into both polynucleotide adenine and guanine of sarcoma 180 was depressed 90% or more...

We used the LYS2 gene mutational system to study mutation specificity of the base analog 6-N-hydroxylaminopurine (HAP) in yeast. We characterized phenotypes of mutations using codon-specific nonsense suppressors and the test employing inactivation of the release factor Sup35 due to overexpressio...

Base analog 6-N-hydroxylaminopurine is a potent mutagen in variety of prokaryotic and eukaroytic organisms. In the review, we discuss recent results of the studies of HAP mutagenic activity, genetic control and specificity in bacteria and yeast with the emphasis to the mechanisms protecting livi...

Genetic control of mutagenesis by the base analog 6-N-hydroxylaminopurine (HAP) was studied in a set of isogenic yeast strains carrying null or point mutations in DNA repair and replication genes. Null alleles of the PMS1, RAD6, REV3 and RAD52 genes did not affect HAP mutagenesis. Defects in 3′...

The enzymatic N-hydroxylation of the purine base adenine to the genotoxic and mutagenic compound 6-N-hydroxylaminopurine is reported for the first time. Adenine was N-oxygenated in vitro by aerobic incubations with 3-methylcholanthrene or isosafrole induced microsomal fractions of rat liver homo...

The genotoxic and mutagenic compound 6-N-hydroxylaminopurine (HAP) can be detoxified in vitro by enzymatic N-reduction to adenine. This reaction is catalysed by both rat and rabbit liver cytosolic fractions. The formation of adenine was monitored using HPLC. Subcellular distribution of the activ...

The activity of a base analog (6-N-hydroxylaminopurine, HAP) has been tested on Aspergillus nidulans. In germinating haploid conidia HAP is a strong mutagen, while it does not have any activity in resting conidia. Moreover, HAP does not increase the frequency of recombination in germinating coni...

Activation of the nuclear farnesoid X receptor (FXR) which acts as cellular bile acid sensor has been validated as therapeutic strategy to counter liver disorders such as non-alcoholic steatohepatitis by the clinical efficacy of obeticholic acid. FXR antagonism, in contrast, is less well studied...