Two series of aromatic hydrazone derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety (7a–r, 8a–i, 12a–b, 13a–c, 16a–d and 17a–e) were designed, synthesized and evaluated for the IC50 values against four cancer cell lines (A549, HepG2, MCF-7and PC-3). Two selected compounds (7c and 17e) we...
Human neutrophil elastase (HNE) is a potent serine protease belonging to the chymotrypsin family. It is an important target for the development of novel and selective inhibitors for the treatment of inflammatory diseases, especially pulmonary pathologies. Here, we report the synthesis and biolog...
C.I.Pigment Yellow 155 (Y 155) is an important bisacetoacetarylide disazo yellow pigment with a unique structure, which has the potential to be an alternative for benzidine yellow pigments due to its superior solvent resistance and light fastness. It is essential to investigate the crystal struc...
Several caspases have been implicated in the pathogenesis of Huntington’s disease (HD); however, existing caspase inhibitors lack the selectivity required to investigate the specific involvement of individual caspases in the neuronal cell death associated with HD. In order to explore the potent...
Regioselective bromination of the title biphenyl 1 at the 3 and 3′ positions and simultaneous desymmetrization of the biphenyl has been achieved. Metal–halide exchange at the 3,3′ positions facilitated the introduction of functional groups in good yield. Regioselective reduction was obtained ...
A novel trichromophoric assembly was synthesized, where two molecules of 7-alkoxy-4-methylcoumarin, acting as energy donors, were linked at a fixed distance and controlled geometry to an energy-acceptor bis(alkylaminostyryl) unit. Resonance energy transfer between the two different species was d...
The spectral characteristics of 1,4-bis[β-(4-quinolyl)vinyl]benzene (B4QVB) have been investigated in different media. Both fluorescence and photoisomerization quantum yields have been determined in different organic solvents. The photoisomerization quantum yield is very small compared to the f...
The possible metabolic activation of the antineoplastic agent N,N-di-(2-chloroethyl) aniline (aniline mustard) is discussed. Conversion of aniline mustard into the glucuronide (p-di-2-chloroethylaminophenyl-β-d-glucopyranosid)uronic acid was mediated by a rat liver homogenate containing the app...
The transfer coefficients of tetra- and hexachlorobiphenyls (PCB-54; -80; -155; and -169), HCB and 4,4′-DDE between milk and blood were monitored for eight weeks in sheep previously administered with these compounds by intramuscular injection. Analyses were performed by high resolution gas chro...
The use of 1,1′-(2,2,2-Trichloro-1,1-ethanediyl)bis(4-chlorobenzene) (DDT) as a pesticide for the control of insects vectors responsible for the spread of many life threatening diseases was officially banned in 1972 by the United States Environmental Protection Agency (USEPA). It was banned thr...
This paper describes an isotope dilution GC/MS technique for the analysis of low-partsper-trillion (ppt) concentrations of 4,4′-DDT, 4,4′-DDD, and 4,4′-DDE in waters and soils. These pesticides are known to be pervasive and dangerous. Known amounts of stable labeled isotopes such as 4,4′-DDT...
Semipermeable membrane devices (SPMDs) spiked with the performance reference compound PCB29 were deployed 6.1 m above the sediments of Lake Chelan, Washington, for a period of 27 d, to estimate the dissolved concentrations of 4,4′-DDT, 4,4′-DDE, and 4,4′-DDD. Water concentrations were estimat...
IntroductionSeveral epidemiological studies have reported that some organochlorine compounds (OCs), such as polychlorobiphenyls (PCBs) and 1,1-dichloro-2,2-bis(4-chlorophenyl)ethylene (4,4′-DDE), may alter thyroid function.
Wastes from the world's largest manufacturer of DDT (1-chloro-4-[2,2,2-trichloro-1-(4-chlorophenyl)ethyl]benzene) were released into the Los Angeles County municipal sewer system from 1947 to 1971. Following primary treatment, the effluent was discharged through a submarine outfall system w...
4,4′-DDT and 4,4′-DDE are widespread environmental contaminants that cause eggshell thinning in birds, altered sex ratios in the American alligator, and changes in the anal–genital distance in rodents. These contaminants are known to cause some of their toxicity by altering steroid receptor-m...
4,4′-Dichlorodiphenyltrichloroethane (DDT), a chlorinated hydrocarbon insecticide, was extensively used in the 1940s and 1950s. DDT is mainly metabolically converted into 4,4′-dichlorodiphenyldichloroethylene (DDE). Even though most countries banned DDT in the 1970s, due to the highly lipophil...
There is a current tendency to develop and apply environmentally friendly techniques that meet the requirements of green analytical chemistry as an alternative to conventional analytical methods. For toxicity evaluation, these alternatives may be found in bioassays such as Tradescantia. This tec...
The role of the glutamatergic system in the convulsant and proconvulsant action of a mitochondrial toxin, 3-nitropropionic acid, was studied in mice. The occurrence of 3-nitropropionic acid-induced seizures was inhibited by the α-amino-2,3-dihydro-5-methyl-3-oxo-isoxazole-propionate (AMPA)/kain...
The behavioural and convulsant effects of imipenem (Imi), a carbapenem derivative, were studied after intraperitoneal (i.p.) or intracerebroventricular (i.c.v.) administration in DBA/2 mice, a strain genetically susceptible to sound-induced seizures. The anticonvulsant effects of some excitatory...
(1-Trimethylsilanylmethyl-vinyl)-phosphonic esters are synthesised via Wittig–Horner reactions starting from methylenediphosphonic esters. The reactions of (1-trimethylsilanylmethyl-vinyl)-phosphonic esters with NsONHCO2Et and CaO, produce α-methylene N-(ethoxycarbonyl) β-amino phosphonic est...
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