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Tertiary Amines (tertiary + amine)
Terms modified by Tertiary Amines Selected AbstractsHybrid Inorganic-Organic Materials Carrying Tertiary Amine and Thiourea Residues Tethered on Mesoporous Silica Nanoparticles: Synthesis, Characterization, and Co-Operative CatalysisADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 1-2 2009Alessandra Puglisi Abstract Mesoporous silica nanoparticles carrying different loadings of tertiary amine and thiourea residues (residues ratios 53/47, 68/32, and 22/78, respectively) were synthesized by the co-condensation method and fully characterized by CP MAS NMR, powder XRD, SEM, BET, BJH and FT-IR techniques. These materials were tested as bifunctional catalysts in the conjugate addition of acetylacetone to 2-nitrostyrene, a reaction that under solvent-free conditions occurred in quantitative yield. By carrying out several experiments with the bifunctional catalysts featuring different molar ratios of active sites, and with different combinations of monofunctional supported and non-supported catalyst, the co-operativity of the tertiary amine and thiourea residues in catalyzing the reaction was demonstrated. The use of the bifunctional catalyst was extended to the addition of acetylacetone to an activated imine. Catalyst recycling for a total of three reaction cycles was demonstrated without significant erosion of activity. [source] Tertiary Amine Mediated Tandem Cross-Rauhut,Currier/Acetalization Reactions: Access to Functionalized Spiro-3,4-Dihydropyrans,ANGEWANDTE CHEMIE, Issue 51 2009Weijun Yao ,-Protonentransfer ermöglichte die hoch selektive Titelreaktion, bei der cyclische ,-Halogenenale 1 mit ,,,-ungesättigten ,-Ketoestern 2 zu funktionalisierten Spiro-3,4-dihydro-2H -pyranen 3 reagieren, in deren Gerüst ein ,-quartäres Kohlenstoffzentrum und eine Vinylhalogenidgruppe benachbart sind. DBU=1,8-Diazabicyclo[5.4.0]undec-7-en, Tos=4-Toluolsulfonyl. [source] ChemInform Abstract: An Effective Kinetic Resolution of Racemic Secondary Benzylic Alcohols Using 3-Pyridinecarboxylic Anhydride and a Chiral Acyl-Transfer Catalyst in the Absence of Tertiary Amine.CHEMINFORM, Issue 21 2010Kenya Nakata Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Tertiary Amine Mediated Tandem Cross-Rauhut,Currier/Acetalization Reactions: Access to Functionalized Spiro-3,4-dihydropyrans.CHEMINFORM, Issue 17 2010Weijun Yao Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: An Unexpected Diethyl Azodicarboxylate Promoted Dehydrogenation of Tertiary Amine and Tandem Reaction with Sulfonyl Azide.CHEMINFORM, Issue 8 2009Xiaoliang Xu Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Heterogeneously Catalyzed Oxidative Cyanation of Tertiary Amines with Sodium Cyanide/Hydrogen Peroxide using Polymer-Supported Iron(II) Phthalocyanines as CatalystADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 8 2010Sweety Singhal Abstract The first report on heterogeneously catalyzed oxidative cyanation of various tertiary amines to the corresponding ,-amino nitriles with high yields and selectivity by using hydrogen peroxide oxidant in presence of sodium cyanide and Fe(II) phthalocyanine supported on a polymer as catalyst is described. The present method has the added benefits of facile recovery of the catalyst from the reaction mixture and its subsequent use without further activation. Consistent catalytic activity with no metal leaching was observed during this course. [source] ChemInform Abstract: Heterogeneously Catalyzed Oxidative Cyanation of Tertiary Amines with Sodium Cyanide/Hydrogen Peroxide Using Polymer-Supported Iron (II) Phthalocyanines as Catalyst.CHEMINFORM, Issue 41 2010Sweety Singhal Abstract The catalyst can be easily recovered and reused for at least five times without any loss of activity and metal leaching. [source] ChemInform Abstract: Platinum-Catalyzed Michael Addition and Cyclization of Tertiary Amines with Nitroolefins by Dehydrogenation of ,,,-sp3 C,H Bonds.CHEMINFORM, Issue 35 2010Xiao-Feng Xia Abstract Mild, one-pot methods to prepare trisubstituted enamines and chromanopiperidines are reported. [source] ChemInform Abstract: Novel Oxidation Reaction of Tertiary Amines with Osmium Tetroxide.CHEMINFORM, Issue 3 2010Hideaki Fujii Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Ruthenium-Catalyzed Oxidative Cyanation of Tertiary Amines with Molecular Oxygen or Hydrogen Peroxide and Sodium Cyanide: sp3 C,H Bond Activation and Carbon,Carbon Bond Formation.CHEMINFORM, Issue 51 2008Shun-Ichi Murahashi Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Selective Synthesis of Secondary and Tertiary Amines by Cp*Iridium-Catalyzed Multialkylation of Ammonium Salts with Alcohols.CHEMINFORM, Issue 26 2008Ryohei Yamaguchi Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Ruthenium-Catalyzed Oxidative Cyanation of Tertiary Amines with Hydrogen Peroxide and Sodium Cyanide.CHEMINFORM, Issue 7 2006Shun-Ichi Murahashi Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access the actual ChemInform Abstract, please click on HTML or PDF. [source] The Titanocene-Catalyzed Reduction of Acetamides to Tertiary Amines by PhMeSiH2.CHEMINFORM, Issue 18 2005Kumaravel Selvakumar No abstract is available for this article. [source] ChemInform Abstract: Palladium Catalyzed 3-Component Cascade Synthesis of Bis(2-arylallyl) Tertiary Amines from Aryl Iodides, Allene and Primary Amines.CHEMINFORM, Issue 2 2002Xinjie Gai Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Reactions of Alkyl, Benzyl, and Stannyl Halides with Lewis Acid Complexed ,-Lithiated Tertiary Amines.CHEMINFORM, Issue 28 2001Satinder V. Kessar Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Diastereoselective Tandem Addition,Cyclization Reactions of Unsaturated Tertiary Amines Initiated by Photochemical Electron Transfer (PET).CHEMINFORM, Issue 17 2001Samuel Bertrand Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Bifunctional Heterogeneous Catalysis of Silica,Alumina-Supported Tertiary Amines with Controlled Acid,Base Interactions for Efficient 1,4-Addition ReactionsCHEMISTRY - A EUROPEAN JOURNAL, Issue 41 2009Ken Motokura Dr. Abstract We report the first tunable bifunctional surface of silica,alumina-supported tertiary amines (SA,NEt2) active for catalytic 1,4-addition reactions of nitroalkanes and thiols to electron-deficient alkenes. The 1,4-addition reaction of nitroalkanes to electron-deficient alkenes is one of the most useful carbon,carbon bond-forming reactions and applicable toward a wide range of organic syntheses. The reaction between nitroethane and methyl vinyl ketone scarcely proceeded with either SA or homogeneous amines, and a mixture of SA and amines showed very low catalytic activity. In addition, undesirable side reactions occurred in the case of a strong base like sodium ethoxide employed as a catalytic reagent. Only the present SA-supported amine (SA,NEt2) catalyst enabled selective formation of a double-alkylated product without promotions of side reactions such as an intramolecular cyclization reaction. The heterogeneous SA,NEt2 catalyst was easily recovered from the reaction mixture by simple filtration and reusable with retention of its catalytic activity and selectivity. Furthermore, the SA,NEt2 catalyst system was applicable to the addition reaction of other nitroalkanes and thiols to various electron-deficient alkenes. The solid-state magic-angle spinning (MAS) NMR spectroscopic analyses, including variable-contact-time 13C cross-polarization (CP)/MAS NMR spectroscopy, revealed that acid,base interactions between surface acid sites and immobilized amines can be controlled by pretreatment of SA at different temperatures. The catalytic activities for these addition reactions were strongly affected by the surface acid,base interactions. [source] Chiral NMR discrimination of amines: Analysis of secondary, tertiary, and prochiral amines using (18-crown-6)-2,3,11,12-tetracarboxylic acid,CHIRALITY, Issue 3-4 2008Ann E. Lovely Abstract Enantiomeric discrimination is observed in the 1H and 13C NMR spectra of secondary and tertiary amines in the presence of (,)-(18-crown-6)-2,3,11,12-tetracarboxylic acid (1). Nonequivalence of the resonances of prochiral nuclei in primary and secondary amines is also observed when they associate with 1. The amines are added in their neutral form and are protonated by the carboxylic acid groups of 1 to produce the corresponding ammonium and carboxylate ions. Secondary amines associate with 1 through two hydrogen bonds and an ion pair interaction. Tertiary amines can only form one hydrogen bond to accompany the ion pairing. Chiral discrimination in the 1H and 13C NMR spectra of a series of aryl-containing secondary amines is of sufficient magnitude to determine enantiomeric purities. The discrimination in the spectra of tertiary amines with 1 is smaller, but 13C NMR spectra provided enough distinction for the determination of enantiomeric purity. Chirality, 2008. © 2007 Wiley-Liss, Inc. [source] Estimation of Ion-Pairing Constants in Plasticized Poly(vinyl chloride) Membranes Using Segmented Sandwich Membranes TechniqueELECTROANALYSIS, Issue 17-18 2009Vladimir Abstract Segmented sandwich membrane method was used to determine ion-pairing constants for four cationic sites: tris-(2,3,4-dodecyloxy)benzenetrimethylammonium, tris-(2,3,4-dodecyloxy)benzenedimethyloctylammonium, tris-(2,3,4-dodecyloxy)benzenemethyldioctylammonium, and dimethyldioctadecylammonium with chloride, bromide, nitrate, benzene sulfonate, trichloroacetate, thiocyanate, perchlorate and picrate, as well as ion-pairing constants for two anionic sites: tetraphenylborate and tris-(2,3,4-octyloxy)benzenesulfonate with dimedrol, quinine, anapriline, and amantadine cations in poly(vinyl chloride) membranes plasticized with 2-nitrophenyl octyl ether. Ion association constants of anions with quaternary ammonium sites regularly increase from picrate to chloride along with reduction of the anion radius and with improvement of site exchanger center steric accessibility. Ion association constants of amine cations with tris-(2,3,4-octyloxy)benzenesulfonate are several orders higher than those with tetraphenylborate and regularly increase from tertiary amine to primary one. [source] Combinations of Acidic and Basic Monodentate Binaphtholic Phosphites as Supramolecular Bidentate Ligands for Enantioselective Rh-Catalyzed HydrogenationsEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 15 2009Luca Pignataro Abstract A small library of chiral BINOL-derived monodentate phosphites containing either a carboxylic acid (-COOH, A1,A3) or a tertiary amine (-NMe2, B1,B4) was synthesized. The ligand combinations were screened in the enantioselective rhodium-catalyzed hydrogenation of methyl 2-acetamidoacrylate. The heterocombinations of the amine-derived phosphite (R)- B2 and of a carboxylic-phosphite [(R)- A1, (R)- A2, (R)- A3] displayed a slightly higher level of enantioselectivity compared to the corresponding homocombinations [up to 90,% ee using (R)- A1/(R)- B2]. The nature and extent of the interaction between the acidic and basic ligands in the rhodium complexes were studied by IR and 31P-NMR spectroscopy. The formation of an intramolecular salt in the Rh-heterocomplex, between the carboxylic acid and the tertiary amine, was suggested by the IR spectra. The selective formation of the Rh-heterocomplex was quantitatively assessed by 31P-NMR spectroscopy, using a modified acidic ligand (R)- A1-Me. In this way, a moderate (ca. 70:30) heterocomplex/homocomplexes ratio was determined.(© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009) [source] Molecular Library Obtained by Allene Insertion into the Pd,C Bond of Cyclopalladated Complexes: Biological and Pharmacological EvaluationEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 8 2004Claude Sirlin Abstract A minilibrary of cationic N-heterocycles has been prepared and evaluated. The potential for the preparation was a result of the high versatility of palladium-mediated chemistry. The synthesis of the novel molecules was based on intramolecular quaternization of tertiary amine attached allylpalladium complexes. The steric and electronic factors of the reaction are discussed. The structures of the synthesized molecules made them candidates for precise biological and pharmacological evaluations. Of the various N-heterocyclic compounds, 2,2-dimethyl-3-methylenenaphtho[def]quinolizinium showed antibacterial activity at micromolar concentrations. This compound also proved to be a nanomolar competitive antagonist for the channel site of the nicotinic acetylcholine receptor. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004) [source] Bifunctional Thiourea-Catalyzed Asymmetric Addition of Anthrones to MaleimidesADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 7 2010Alex Zea Abstract For the first time, the addition of anthrones to maleimides catalyzed by bifunctional thiourea catalysts is reported. The thiourea moiety is able to activate the maleimide and the tertiary amine deprotonates the anthrone, furnishing the final Diels,Alder or Michael adducts in excellent yields and enantioselectivities. [source] Hybrid Inorganic-Organic Materials Carrying Tertiary Amine and Thiourea Residues Tethered on Mesoporous Silica Nanoparticles: Synthesis, Characterization, and Co-Operative CatalysisADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 1-2 2009Alessandra Puglisi Abstract Mesoporous silica nanoparticles carrying different loadings of tertiary amine and thiourea residues (residues ratios 53/47, 68/32, and 22/78, respectively) were synthesized by the co-condensation method and fully characterized by CP MAS NMR, powder XRD, SEM, BET, BJH and FT-IR techniques. These materials were tested as bifunctional catalysts in the conjugate addition of acetylacetone to 2-nitrostyrene, a reaction that under solvent-free conditions occurred in quantitative yield. By carrying out several experiments with the bifunctional catalysts featuring different molar ratios of active sites, and with different combinations of monofunctional supported and non-supported catalyst, the co-operativity of the tertiary amine and thiourea residues in catalyzing the reaction was demonstrated. The use of the bifunctional catalyst was extended to the addition of acetylacetone to an activated imine. Catalyst recycling for a total of three reaction cycles was demonstrated without significant erosion of activity. [source] Recovery of pyruvic acid with weakly basic polymeric sorbentsJOURNAL OF CHEMICAL TECHNOLOGY & BIOTECHNOLOGY, Issue 5 2008Shaokai Huang Abstract BACKGROUND: Carboxylic acids are among the most important substances that can be manufactured from biomass. However, the recovery of carboxylic acids from fermentation broths presents a challenging separation problem. To avoid the production of waste salts and net consumption of chemicals in the calcium carboxylate salt process, the use of reversible chemical complexation with polymeric sorbents and extractants is attractive for carboxylic acid recovery. Pyruvic acid is widely used in the manufacture of medicines, pesticides and foodstuffs and can be produced by fermentation. Since the acidity of pyruvic acid (pKa = 2.49) is stronger than that of normal carboxylic acids, and as few reports on the recovery of pyruvic acid are available, the sorption of pyruvic acid from aqueous solution on two types of weakly basic polymeric sorbent, tertiary amine D301R and primary amine D392, was investigated over a wide pH range and at various salt (MgSO4) concentrations. RESULTS: Overloading adsorption of pyruvic acid on both weakly basic polymeric sorbents occurred, with the overloading of D392 being greater than that of D301R. The adsorption of pyruvic acid on both sorbents was greatly affected by the solution pH and the salt concentration in the aqueous phase. An overloading model was able to predict the experimental uptake data very well. CONCLUSION: Solution pH is one of the most important operating conditions, and both polymeric sorbents D392 and D301R can be used to recover pyruvic acid from dilute aqueous solution with high efficiency at a solution pH around 2. The uptake by D392 is greater than that by D301R owing to steric hindrance of the tertiary amine. Copyright © 2008 Society of Chemical Industry [source] Catalytic kinetics of quaternary ammonium poly(styrene- co -methylstyrene) resinAICHE JOURNAL, Issue 7 2006Ho-Shing Wu Abstract The catalytic kinetics and synthesis of poly(styrene- co -chloromethylstyrene) resin of different degrees of crosslinkages and ring substitutions were investigated by copolymerizing styrene and chloromethylstyrene through crosslinking with divinylbenzene. Poly(styrene- co -chloromethylstyrene) quaternary ammonium salt was obtained with activating poly(styrene- co -chloromethylstyrene) resin with tertiary amine. More than 20 types of poly(styrene- co -chloromethylstyrene) quaternary ammonium catalyst were prepared, with reaction conditions including immobilized time (0.125,4 days), concentration of tertiary amine (0.1,2 kmol/m3), kinds of solvents in immobilization (methanol, ethyl alcohol, and DMF), and kinds of tertiary amines (trimethylamine, triethylamine, tripropylamine, tri- n -butylamine, tri- n -pentylamine, tri- n -hexylamine, and tri- n -octylamine). These catalysts were used to achieve the optimum allylation of phenol. The reactions were conducted and studied individually with either equal mole or equal weight of catalyst. The best reactivity for the allylation of phenol was obtained when the structure of the quaternary ammonium catalyst was 10% degree of ring substitution and 2% degree of crosslinkage activating with trihexylamine. The turnover number and the effectiveness factor were also calculated. © 2006 American Institute of Chemical Engineers AIChE J, 2006 [source] Frontal polymerization with monofunctional and difunctional ionic liquid monomersJOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 13 2007Zulma Jiménez Abstract For the first time, we studied frontal polymerization with ionic liquid monomers. We synthesized a series of compounds from the neutralization reaction between trialkylamines (tributylamine, trihexylamine, trioctylamine, and (2-dimethylamino)ethyl methacrylate) and acrylic or methacrylic acid. For the ionic liquids prepared from the unreactive amines, frontal polymerization could not be achieved without the addition of a diacrylate. With the addition of a diacrylate, the front velocities were slower than for dodecyl acrylate (with the diacrylate), a compound of comparable molecular weight. Monomers prepared from the (2-dimethylamino)ethyl methacrylate could support frontal polymerization alone but the front velocities were lower than dodecyl (meth)acrylate. These results are contrasted with recent results of Jiménez et al. for room temperature kinetics. Finally, the polymers prepared were comparable to those prepared by batch curing at 75 °C except for the monomethacrylate ionic liquid, which lost some tertiary amine by dissociation and evaporation. © 2007 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 45: 2745,2754, 2007 [source] Photopolymerization of 1,6-hexanedioldiacrylate initiated by three-component systems based on N -arylphthalimidesJOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 16 2004T. Brian Cavitt Abstract Three-component photoinitiators comprised of an N -arylphthalimide, a diarylketone, and a tertiary amine were investigated for their initiation efficiency of acrylate polymerization. The use of an electron-deficient N -arylphthalimide resulted in a greater acrylate polymerization rate than an electron-rich N -arylphthalimide. Triplet energies of each N -arylphthalimide, determined from their phosphorescence spectra, and the respective rate constants for triplet quenching by the N -arylphthalimide derivatives (acquired via laser flash photolysis) indicated that an electron,proton transfer from an intermediate radical species to the N -arylphthalimide (not energy transfer from triplet sensitization) is responsible for generating the initiating radicals under the conditions and species concentrations used for polymerization. © 2004 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 42: 4009,4015, 2004 [source] Liquid-crystalline thermosets by the curing of dimeric liquid-crystalline epoxyimine monomers with 2,4-toluene diisocyanateJOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 16 2003David Ribera Abstract We studied the curing processes of several series of dimeric liquid-crystalline epoxyimine monomers with 2,4-toluene diisocyanate (TDI) alone or with added catalytic proportions of 4-(N,N -dimethylamino)pyridine. We obtained isotropic materials or liquid-crystalline thermosets with different degrees of order, which depended on the structures of the monomers. To fix ordered networks, we had to do the curing in two steps when TDI was used alone as the curing agent. However, when a tertiary amine was added in catalytic proportions, the ordered networks were fixed in just one step. In this way, we were able to fix both nematic and smectic mesophases. The significance of the polarization of the mesogen for obtaining liquid-crystalline thermosets was demonstrated. © 2003 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 41: 2521,2530, 2003 [source] Factors influencing the adsorption of stabilizers onto carbon black: Flow microcalorimetry studiesJOURNAL OF VINYL & ADDITIVE TECHNOLOGY, Issue 2 2000J. M. Peñta The surface activity of various kinds of carbon black toward phenolic antioxidants and hindered amine light stabilizers (HALS) was examined by using flow microcalorimetry (FMC). Phenolic hydroxyl and ester groups were found to be the moieties responsible for the adsorption activity of primary phenolic antioxidants onto the carbon black surfaces. Furthermore, a difference in the degree of phenolic hydroxyl hindrance by alkyl groups was found to be the main factor affecting the adsorption activity of the phenol group. A difference in the degree of substitution of the piperidine amine, as well as the number and type of functionality per molecule, are important factors that were found to influence the adsorption activity of HALS. Data from adsorption studies using model compounds, some of which represented functional portions of the stabilizer molecules, reflected behavior sin ilar to that observed with the stabilizers. In addition, these latter results showed that FMC analysis can yield potentially useful information beyond that given by the usual parameters such as BET surface area, I2, DBP, and CTAB adsorption values. Differences in the behavior between types of carbon black were evident and showed that the specific surface area is not the most important factor in the adsorption/desorption activity, but also the chemical nature of the surface. From the activity observed for model compounds, it was deduced that the presence of secondary and tertiary amine in the backbone and branch structures also has an important role in the adsorption activity of polymeric HALS. In general, the observed quantities can be related to the values of adsorption/desorption energy and to the molar mass of the probe. [source] Evaluation of mutagenic and antimutagenic properties of some bioactive xanthone derivatives using Vibrio harveyi testLETTERS IN APPLIED MICROBIOLOGY, Issue 3 2010Abstract Aims:, Drug safety evaluation plays an important role in the early phase of drug development, especially in the preclinical identification of compounds' biological activity. The Vibrio harveyi assay was used to assess mutagenic and antimutagenic activity of some aminoalkanolic derivatives of xanthone (1,5), which were synthesized and evaluated for their anticonvulsant and hemodynamic activities. Methods and Results:, A novel V. harveyi assay was used to assess mutagenic and antimutagenic activity of derivatives of xanthone 1,5. Two V. harveyi strains were used: BB7 (natural isolate) and BB7M (BB7 derivative containing mucA and mucB genes on a plasmid pAB91273, products of these genes enhance error-prone DNA repair). According to the results obtained, the most beneficial mutagenic and antimutagenic profiles were observed for compounds 2 and 3. A modification of the chemical structure of compound 2 by the replacement of the hydroxy group by a chloride improved considerably the antimutagenic activity of the compound. Thus, antimutagenic potency reached a maximum with the presence of tertiary amine and chloride atom in the side chain. Conclusions:, Among the newly synthesized aminoalkanolic derivatives of xanthone with potential anticonvulsant properties, there are some compounds exhibiting in vitro antimutagenic activity. In addition, it appears that the V. harveyi assay can be applied for primary mutagenicity and antimutagenicity assessment of compounds. Significance and Impact of the Study:, The obtained preliminary mutagenicity and antimutagenicity results encourage further search in the group of amino derivatives of xanthone as the potential antiepileptic drugs also presenting some antimutagenic potential. Furthermore, V. harveyi test may be a useful tool for compounds safety evaluation. [source] | |||||||||||||||||||||||||||||||