Search results for " DERIVATIVES"
showing 10 items of 391 documents
Multidrug resistance reverting activity and antitumor profile of new phenothiazine derivatives
2008
Abstract A series of easily affordable phenothiazine derivatives bearing a rigid but-2-ynyl amino side chain were synthesized and tested to evaluate the MDR reverting activity and full antitumor profile. Some compounds endowed with remarkable MDR reverting effect were identified, and the most active one ( 6c ) was shown to increase doxorubicin retention in multidrug resistant cells, suggesting a direct interaction with P-glycoprotein. Furthermore, a broad range of cellular activities were observed for different compounds. In particular, the ability of some derivatives to induce antiproliferative effects on resistant cell lines and to interfere with the G 1 phase of the cell cycle, a phase u…
Development of a versatile, easy and rapid atmospheric monitor for benzene, toluene, ethylbenzene and xylenes determination in air
2009
Abstract A new procedure for the passive sampling in air of benzene, toluene, ethylbenzene and xylene isomers (BTEX) is proposed. A low-density polyethylene layflat tube filled with a mixture of solid phases provided a high versatility tool for the sampling of volatile compounds from air. Several solid phases were assayed in order to increase the BTEX absorption in the sampler and a mixture of florisil and activated carbon provided the best results. Direct head-space-gas chromatography–mass spectrometry (HS-GC–MS) measurement of the whole deployed sampler was employed for a fast determination of BTEX. Absorption isotherms were used to develop simple mathematical models for the estimation of…
Effects of cyclooxygenase-1/cyclooxygenase-2 inhibition on leukocyte/endothelial cell interactions in the rat mesentery.
2002
Nonsteroidal anti-inflammatory drugs (NSAID) inhibit cyclooxygenase activity and cause gastrointestinal damage in part by promoting leukocyte accumulation in the mucosa. Our aim was to evaluate the effects of selective blockade of the isoenzymes cyclooxygenase-1 and cyclooxygenase-2 on leukocyte adhesion in vivo. Leukocyte/endothelial cell interactions were examined in rat mesenteric venules before and after treatment with indomethacin, SC-560 (5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-trifluoromethylpyrazole, cyclooxygenase-1 inhibitor), DFP (5,5-dimethyl-3-(2-propoxy)-4-(4-methanesulfonyl)-2(5H)-furanone, cyclooxygenase-2 inhibitor), or SC-560 plus DFP (20 mg/kg, i.v. each). Indomethacin i…
Oxidative stress induces distinct physiological responses in the two Trebouxia phycobionts of the lichen Ramalina farinacea
2010
† Background and Aims Most lichens form associations with Trebouxia phycobionts and some of them simultaneously include genetically different algal lineages. In other symbiotic systems involving algae (e.g. reef corals), the relative abundances of different endosymbiotic algal clades may change over time. This process seems to provide a mechanism allowing the organism to respond to environmental stress. A similar mechanism may operate in lichens with more than one algal lineage, likewise protecting them against environmental stresses. Here, the physiological responses to oxidative stress of two distinct Trebouxia phycobionts (provisionally named TR1 and TR9) that coexist within the lichen R…
The organic air pollutant cumene hydroperoxide interferes with NOantioxidant role in rehydrating lichen
2013
Organic pollutants effects on lichens have not been addressed. Rehydration is critical for lichens, a burst of free radicals involving NO occurs. Repeated dehydrations with organic pollutants could increase oxidative damage. Our aim is to learn the effects of cumene hydroperoxide (CP) during lichen rehydration using Ramalina farinacea (L.) Ach., its photobiont Trebouxia spp. and Asterochloris erici. Confocal imaging shows intracellular ROS and NO production within myco and phycobionts, being the chloroplast the main source of free radicals. CP increases ROS, NO and lipid peroxidation and reduces chlorophyll autofluorescence, although photosynthesis remains unaffected. Concomitant NO inhibit…
Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis
2019
This paper describes an optimization strategy of the highly active vinyl ketone 3 which was recognized as a strong inhibitor of rhodesain of Trypanosoma brucei rhodesiense, endowed with a ksecond v...
Radical salts of TTF derivatives with the metal-metal bonded [Re2Cl8]2- anion
2008
Abstract Four new salts of the radical cations of TMTSF (tetramethyltetraselenafulvalene), TMTTF (tetramethyltetrathiafulvalene), BEDT-TTF (bisethylenedithiotetrathia-fulvalene) (ET) and o-Me2TTF (o-4,4′-dimethyltetrathiafulvalene) with the metal–metal bonded dianion [Re2Cl8]2− were synthesized, and their structures and physical properties investigated. The structures of these semiconducting salts feature one-dimensional stacking of the donor molecules interleaved with [Re2Cl8]2− anions and interstitial solvent molecules.
A Short Synthesis of Polysubstituted Pyrrolidines via α-(Alkylideneamino)nitriles
2004
α-(Alkylideneamino)nitriles can be deprotonated under mild conditions. Their conjugated anions react with enones in a 1,4-addition to yield δ-keto-α-(alkylideneamino)nitriles which in turn can be reduced to form pyrrolidines in a one-pot reaction sequence.
New Fluorinated 1,3-Vinylogous Amidines as Versatile Intermediates: Synthesis of Fluorinated Pyrimidin-2(1H)-ones.
2006
The condensation of the azaenolates derived from readily available ketimines with fluorinated nitriles offers an efficient and straightforward entry to new fluorinated 1,3-vinylogous amidines. These versatile compounds, in turn, react with triphosgene to yield new fluorinated pyrimidin-2(1H)-ones in high yields.
An In Vitro Experiment for Postmortem Vascular Permeation. The Passage of Morphine and Morphine Glucuronides Across a Vascular Wall
1997
A venous blood sample taken at autopsy cannot be considered to represent the antemortem blood concentration of a particular substance. Autolytic processes cause disintegration and increasing permeability of the physiological and anatomical barriers such as vascular walls and lead to changes in substance concentrations. In the present study, the experimental design represents an in vitro postmortem simulation of a drug substance crossing a venous wall. The postmortem behavior of morphine, morphine-3- and morphine-6-glucuronide was investigated. A Chien-Valia-diffusion chamber with a patch of inferior vena cava as diffusion barrier was used. For optimal simulation of postmortem events, vein s…