Search results for "Amidine"
showing 10 items of 60 documents
Reactions of platinum(iv)-bound nitriles with isomeric nitroanilines: addition vs. substitution
2012
The platinum(IV) complex trans-[PtCl(4)(EtCN)(2)] reacts smoothly and under mild conditions with isomeric o-, m- and p-nitroanilines (NAs) yielding two different types of products depending on the NA isomer, viz. the nitroaniline complexes cis/trans-[PtCl(4)(NA)(2)] (cis/trans-1-3) and the amidine species trans-[PtCl(4){NH=C(Et)NHC(6)H(4)NO(2)-m}(EtCN)] (4), trans-[PtCl(4){NH=C(Et)NHC(6)H(4)NO(2)-m}(2)] (5) and trans-[PtCl(4){NH=C(Et)NHC(6)H(4)NO(2)-p}(EtCN)] (6). Complexes 4 and 5 undergo cyclometalation, furnishing mer-[PtCl(3){NH=C(Et)NHC(6)H(3)NO(2)-m}(EtCN)] (7) and mer-[PtCl(3){NH=C(Et)NHC(6)H(4)NO(2)-m}{NH=C(Et)NHC(6)H(3)NO(2)-m}] (8), respectively. Moreover, 8 both in the solid stat…
Lidocaine inhibits potassium efflux and hemolysis in erythrocytes during oxidative stress in vitro.
2000
Lidocaine is a widely used local anesthetic agent. The aim of this work was to study the action of lidocaine on human red blood cells exposed to an oxidative stress in vitro. Blood was obtained from healthy volunteers. After separation from plasma, the erythrocytes were suspended in phosphate buffer. Oxidative stress was induced by incubation with a free radical generator, the 2,2' azobis (2-amidinopropane) hydrochloride (AAPH). Erythrocytes were incubated with or without lidocaine at two concentrations (36.93 and 73.85 microM) and with or without AAPH (20 mM). Electron paramagnetic resonance (EPR) spectroscopy was performed to identify the free radical species generated by AAPH using the s…
Antioxidant Activity of All-trans-retinol in Homogeneous Solution and in Phosphatidylcholine Liposomes
1993
A kinetic quantification of the lipoperoxyl radical-scavenging activity of all-trans-retinol has been carried out in homogeneous solution, when radicals were produced from the oxidation of methyl linoleate in methanol, initiated by the lipid-soluble 2,2′-azobis (2,4-dimethyl-valeronitrile) (AMVN) as well as in a soybean phosphatidylcholine membrane model, in which peroxidation was induced either by AMVN or the hydrophylic 2,2′-azobis(2-amidinopropane)hydrochloride (AAPH). The physical microenvironment contributes to the determination of antioxidant efficiency of all-trans-retinol. In homogeneous solution the kinetic constant kinh is 3.5 × 105 M-1 s-1 and appears of the same order of magnitu…
Phosphine-diène and Salicylamidines ligands : coordination chemistry, catalysis and therapy
2017
The subject of this thesis concerns the development of new ligands, their coordination chemistry, and the synthesis of the corresponding metal complexes for catalysis and therapy.The first part of this work relates to the synthesis of diene-phosphine ligands, their saturated analogs, and the corresponding arene-ruthenium complexes. Arene decoordination allows the formation of a cationic bimetallic complex where the ligand is diène-η4/κ-P coordinated to the ruthenium. These complexes have been applied to atom transfer radical addition (ATRA) of CCl4 to styrene. When harsh reaction conditions are used, the superiority of the “diene” complexes is highlighted comparing to saturated analogs.The …
The brainstem efferent acoustic chiasm in pigmented and albino rats
2015
Abstract The present study examined whether structural peculiarities in the brain-efferent pathway to the organ of Corti may underlie functional differences in hearing between pigmented and albino individuals of the same mammalian species. Pigmented Brown-Norway rats and albino Wistar rats received unilateral injections of an aqueous solution of the retrograde neuronal tracer Fluorogold (FG) into the scala tympani of the cochlea to identify olivocochlear neurons (OCN) in the brainstem superior olivary complex. After five days, brains were perfusion-fixed and brainstem sections were cut and analyzed with respect to retrogradely labeled neurons. Intrinsic neurons of the lateral system were lo…
Synthesis of Fluorinated and Non-Fluorinated Bicyclic Amidines through Ring-Closing Metathesis
2011
[EN] An efficient method for the synthesis of fluorinated and non-fluorinated imidazoazepines by a ring-closing metathesis reaction as the key step is described. The influence of the fluorine atoms on the preparation of these bicyclic systems is also studied.
Phenoloxidase characterization in vacuolar hemocytes from the solitary ascidian Styela plicata
1995
Phenoloxidase (PO) activity was shown in lysates of Styela plicata hemocytes assayed spectrophotometrically by means of L-Dopa oxidation without divalent cations. Trypsin and chymotrypsin pretreatment and preincubation with microbial lipopolysaccharides significantly activated PO, whereas laminarin or zymosan were ineffective. Soybean trypsin inhibitor, tropolone, and phenylthiourea, but not benzamidine, were inhibitors. Finally, hemocytes were separated by a discontinuous Percoll density gradient to determine which cells were active. PO activity was demonstrated, by both biochemical and cytochemical assays, in the separated fraction enriched mainly with the globular granulocytes called mor…
Ammonia Activation by a Nickel NCN-Pincer Complex featuring a Non-Innocent N-Heterocyclic Carbene: Ammine and Amido Complexes in Equilibrium
2015
A Ni0-NCN pincer complex featuring a six-membered N-heterocyclic carbene (NHC) central platform and amidine pendant arms was synthesized by deprotonation of its NiII precursor. It retained chloride in the square-planar coordination sphere of nickel and was expected to be highly susceptible to oxidative addition reactions. The Ni0 complex rapidly activated ammonia at room temperature, in a ligand-assisted process where the carbene carbon atom played the unprecedented role of proton acceptor. For the first time, the coordinated (ammine) and activated (amido) species were observed together in solution, in a solvent-dependent equilibrium. A structural analysis of the Ni complexes provided insig…
A Hyaluronic acid-pentamidine bioconjugate as macrophage mediated drug targeting delivery system for the treatment of Leishmaniasis
2015
Leishmaniasis is still a serious public health problem worldwide, especially in tropical areas where this infectious disease is endemic. The most severe form of the disease (i.e. visceral) can claim victims if left untreated and the few accessible drugs have several drawbacks including major side effects and parenteral administration. In this context, the investigation of new delivery modalities which might reduce the toxicity and increase the bioavailability of the drugs currently on the market represents a valid strategy to counter these problems. Herein we present the development of a macrophage mediated drug targeting delivery system by conjugating the anti-leishmanial drug pentamidine …
Struktur-Wirkungs-Beziehungen bei Histaminanaloga, 13. Mitt.: 5(4)-Cyclisch substituierte Histamine und Nα-Methyl-histamine
1976
Es wird die Darstellung von 5(4)-cyclisch substituierten Histaminen und Nα-Methyl-histaminen durch Cyclisierung von 1-aryl-substituierten 2-Brom-4-phthalimido-butan-1-onen mit Formamid oder Benzamidin und anschliesende Hydrolyse bzw. Reduktion der Zwischenprodukte beschrieben. C-5(4) Cyclic Substituted Histamines and Nα-Methylhistamines The preparation of C-5(4) cyclic substituted histamines and Nα-methylhistamines by cyclisation of 1-aryl-2-bromo-4-phthalimidobutan-1-ones with formamide or benzamidine, followed by hydrolysis or reduction of the intermediates, is described.