A series of novel 1,2-benzothiazine 1,1-dioxide-3-ethanone oxime N-aryl acetamide ether derivatives 7a–h and 9a–h were synthesized starting from sodium salt of saccharin 1 in series of steps. Final compounds 7a–h and 9a–h were evaluated for the anti-inflammatory activity and their ability to...
Herein we report the synthesis of twelve 2,5-substituted 4-(trifluoromethyl)-spirochromeno[4,3-d]pyrimidines (7–10), as well as an evaluation of their analgesic effect in a mouse pain model. The nine new chromeno[4,3-d]pyrimidines (7–9) were synthesized from the cyclocondensation reactions of ...
A useful synthetic route for an initial new series of 2-substituted 4-(trifluoromethyl)-5,6-dihydrobenzo[h]quinazolines (3), as well as an evaluation of their analgesic effect in a mice pain model, is reported. Five new quinazolines were formed from the cyclocondensation reactions of 2,2,2-trifl...
The biosynthetic pathway of 19-noraldosterone (19-noraldo) in isolated rat glomerulosa cells (GC) and fasciculata-reticular cells (FC) was studied by analyzing [14C] pregnenolone metabolism using HPLC and quantification by specific RIA. In GCs, 18,19-dihydroxycorticosterone was detected after 15...
18,19-Dihydroxycorticosterone (18,19(OH)2-B) and 18-hydroxy-1 9-norcorticosterone (18-OH-19-nor-B) measurements were carried out on the urine of patients with primary aldosteronism (PA), essential hypertension (EHT), and liver cirrhosis with (LC, SA ( + )) and without (LC, SA( − )) aldosteronism...
The redox state of molybdopterin cytosine dinucleotide (MCD) from the molybdo-iron-sulfur-flavoprotein CO dehydrogenase of the carboxidotrophic bacterium Hydrogenophaga pseudoflava has been studied. MCD has been purified as the dicarboxamidomethylated derivative (5,6-dihydro-di(cam)MCD) under co...
The specificity of the anti A + N lectin of Moluccella laevis (MLL) was examined by hemagglutination experiments with enzyme-modified human erythrocytes and by inhibition of hemagglutination. In addition, binding to various glycoproteins and inhibition by different sugars and glycoproteins were ...
Publisher SummaryLysyl oxidase activity and the rate of cross-linking must be reduced effectively to cause an increase in the net pool of soluble elastins prior to isolation. This may be achieved by rendering animals nutritionally copper-deficient or lathrytic. The choice of experimental animals...
Biomaterials based upon elastin and elastin-derived molecules are increasingly investigated for their application in tissue engineering. This interest is fuelled by the remarkable properties of this structural protein, such as elasticity, self-assembly, long-term stability, and biological activi...
Elastins encompass the class of protein-based materials derived from the sequence of tropoelastin, the major protein component of native elastic tissue in vertebrates. Biophysical studies of native tropoelastin and tropoelastin-derived sequences have provided insight into the structural mechanis...
Elastin is a protein of the extracellular matrix that contributes significantly to the elasticity of connective tissues. In this study, we examine dynamical and structural modifications of aortic elastin exposed to cholesterol by NMR spectroscopic and relaxation methodologies. Macroscopic measur...
Elastin-like recombinamers (ELRs), which derive from one of the repetitive domains found in natural elastin, have been intensively studied in the last few years from several points of view. In this mini review, we discuss all the recent works related to the investigation of ELRs, starting with t...
Glutathione conjugation has been identified as an important detoxication reaction. However, several glutathione-dependent bioactivation reactions have been identified. Current knowledge on the mechanisms and the possible biological importance of these reactions is discussed in this article. Vici...
The genotoxicity of the glutathione S-conjugates S-(12-dichlorovinyl)glutathione (DCVG), S-(1,2,2-trichlorovinyl)glutathione (TCVG), S-(1,2,3,4,4-pentachlorobutadienyl)glutathione (PCBG) and S-(2-chloroethyl)glutathione (CEG) was investigated in LLC-PK1, a cultured line of porcine kidney cells t...
Many potentially toxic electrophilic xenobiotics and some endogenous compounds are detoxified by conversion to the corresponding glutathione S-conjugate, which is metabolized to the N-acetylcysteine S-conjugate (mercapturate) and excreted. Some mercapturate pathway components, however, are toxic...
The nephrotoxic and nephrocarcinogenic potential of the haloalkenes is associated with the conjugation of the chemicals to l-glutathione. Subsequent processing of the haloalkene glutathione S-conjugates via the cysteine conjugate β-lyase pathway in the mammalian kidney yields nephrotoxic and mu...
Perchloroethene (Per) is a widely used industrial solvent and common environmental contaminant. In rats, long-term inhalation of Per is known to cause a small increase in the incidence of renal tubule cell tumors in males only; renal toxicity is seen in female rats and in both sexes of mice afte...
Suspensions of renal cells from rats and renal mitochondria from rats and mice were used to assess the sex and species dependence of acute toxicity due to perchloroethylene (Perc) and its glutathione conjugate S-(1,2,2-trichlorovinyl)glutathione (TCVG). A marked sex dependence in the acute cytot...
5-Phenyl-3-[(2′R,3′S)-3′-hydroxy-2′-dimethoxymethyltetrahydrofuran-3′-yl]-1,2,4-oxadiazole 10a and its epimer 11a, 5-methyl-3-[(2′R,3′S)-3′-hydroxy-2′-dimethoxymethyltetrahydrofuran-3′-yl]-1,2,4-oxadiazole 10b and its epimer 11b were synthesized from cyanohydrin benzoates 8a, 9a and cy...
An innovative and efficient route to the synthesis of 9,10-dihydro-3-formylphenanthrenes 7 has been delineated through the ring transformation of 2-oxo-4-sec-amino-5,6-dihydro-2H-benzo[h]chromene-3-carbonitriles 4 with methyl glyoxaldimethylacetal 5 to masked 3-dimethoxymethyl-1-sec-amino-9,10-d...
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