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Amine Derivatives (amine + derivative)
Selected AbstractsSynthesis and pp60c-Src Tyrosine Kinase Inhibitory Activities of Novel Indole-3-Imine and Amine Derivatives Substituted at N1 and C5ARCHIV DER PHARMAZIE, Issue 6 2009Zuhal Kiliç Abstract A series of novel 1,3,5-trisubstituted indole derivatives, namely, N -benzyl 5-phenyl indole-3-imine, N -benzyl-5-(p -fluorophenyl)indole-3-imine and their corresponding amine congeners, were designed and synthesized as pp60c-Src tyrosine kinase inhibitors, and their inhibitory activities toward pp60c-Src tyrosine kinase were evaluated by in-vitro kinase assay. Pre-screening at two doses of compounds against kinase target revealed that, except for the N -benzyl-5-phenyl indole imine derivatives 7a,7d, all indole derivatives show the target inhibition at varying levels. Consequently, the compounds, 8c, 8f, 8g, and 8h, were selected for prescreening tests. The dose-response curves for up to six concentrations (250 to 7.8 ,M) of the active compounds were obtained by tyrosine kinase assay and the four-parameter logistic analysis of these data resulted in the IC50s of 4.69, 74.79, 75.06, and 84.23 ,M for compounds 8c, 8f, 8g, and 8h, respectively. Therefore, compound 8c, 1-(1-benzyl-5-phenyl-1H -indole-3-yl)- N -(4-fluorobenzyl)methanamine·HCl, was the promising inhibitor for pp60c-Src, followed by compounds 8g and 8h. Under the same conditions, compound 8f did not provide any reasonable inhibition pattern to be considered as active compound. Therefore, among all four active compounds, compound 8f was not found suitable for further analysis. [source] ChemInform Abstract: One-Pot Synthesis of Highly Substituted Aromatic Amine Derivatives via Pd-Catalyzed Aminobenzannulation Reaction.CHEMINFORM, Issue 48 2009Fa-Rong Gou 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] A General One-Pot, Three-Component Mono N-Alkylation of Amines and Amine Derivatives in Lithium Perchlorate/Diethyl Ether Solution.CHEMINFORM, Issue 32 2005Akbar Heydari Abstract For Abstract see ChemInform Abstract in Full Text. [source] Palladium-Catalyzed Carbonylation of Homoallylic Amine Derivatives in the Presence of a Copper Co-Catalyst.CHEMINFORM, Issue 39 2003Takanori Mizutani Abstract For Abstract see ChemInform Abstract in Full Text. [source] Preparation of Bis(,-trimethylsilylethanesulfonyl)imide and Its Use in the Synthesis of Protected Amine Derivatives.CHEMINFORM, Issue 38 2003David M. Dastrup Abstract For Abstract see ChemInform Abstract in Full Text. [source] Novel Iminium Ion Equivalents Prepared Through C,H Oxidation for the Stereocontrolled Synthesis of Functionalized Propargylic Amine Derivatives.CHEMINFORM, Issue 23 2003James J. Fleming Abstract For Abstract see ChemInform Abstract in Full Text. [source] Investigating Amine Derivatives of Ambruticin VS-5 and VS-4CHEMMEDCHEM, Issue 6 2008Zong-Qiang Tian Dr. Abstract A structure,activity relationship around the amine group of the ambruticin VS series has been developed for antifungal activity. It was shown that the amine can be alkylated through reductive amination without loss of potency. However, if it is converted into either an amide, carbamate, or urea, a significant loss of potency is observed. Of the alkyl amines, small nonpolar groups are optimal for both potency and oral bioavailability. As a result of this study, one compound (KOS-2079) was taken into an animal efficacy model with success. [source] A new strategy for the synthesis of cyclopeptides containing diaminoglutaric acidJOURNAL OF PEPTIDE SCIENCE, Issue 5 2001Tom Bayer Abstract A new synthesis of orthogonally protected diaminoglutaric acid containing peptides using the Ugi four component condensation is presented. To demonstrate that this method is useful to replace cystine by diaminoglutaric acid in biologically interesting peptides, we built up two cyclic somatostatin analogues deriving from Sandostatin and from TT-232. A photolytically cleavable amine derivative of the nitroveratryl type is used for the Ugi four component condensation. Because of a racemic build up of the new stereocentre of the diaminoglutaric acid, and racemization of the isonitrile component, four diastereomeric peptides resulted that were separated by HPLC. The stereochemistry of the cyclopeptides could be easily and unambiguously assigned by chiral gas chromatography and a reference sample of enantiomerically pure (2S,4S)-diaminoglutaric acid. Copyright © 2001 European Peptide Society and John Wiley & Sons, Ltd. [source] Mutagenicity of nitroaromatic degradation compoundsENVIRONMENTAL TOXICOLOGY & CHEMISTRY, Issue 10 2003Ranjit S. Padda Abstract The mutagenicity of 2,4-dinitrotoluene (24DNT), and 2,6-dinitrotoluene (26DNT), and their related transformation products such as hydroxylamine and amine derivatives, which are formed by Clostridium acetobutylicum, were tested in crude cell extracts using Salmonella typhimurium TA100. A previous publication already reported the mutagenic activities of 2,4,6-trinitrotoluene (TNT) and its related hydroxylamine derivatives in this test system. A time course of the mutagenicity during the anaerobic transformation of TNT, 24DNT, and 26DNT was also investigated under the same conditions to compare with the results from the pure compounds. The monohydroxylamino intermediates 2-hydroxylamino-4-nitrotoluene (2HA4NT), 4-hydroxylamino-2-nitrotoluene (4HA2NT) and 2-hydroxylamino-6-nitrotoluene (2HA6NT) formed during anaerobic transformation of dinitrotoluenes were proven to be mutagenic in the Ames test using Salmonella typhimurium TA100. This study reports that 4HA2NT is the most stable derivative, whereas 2HA4NT and 2HA6NT are less stable and these intermediates are mutagenic in the Ames test. Both 24DNT and 26DNT and their final metabolites 2,4-diaminotoluene (24DAT) and 2,6-aminotoluene (26DAT) appeared nonmutagenic. In a time-course study of TNT degradation, the temporal sample containing 85% of 2,4-dihydroxylamino-6-nitrotoluene (24HA6NT) is most mutagenic. These observations suggest that the bioremediation approach for treatment of 24DNT and 26DNT should be carried past the hydroxylamino intermediate. [source] Gold(I)- and Brønsted Acid-Catalyzed Ring-Opening of Unactivated Vinylcyclopropanes with SulfonamidesADVANCED SYNTHESIS & CATALYSIS (PREVIOUSLY: JOURNAL FUER PRAKTISCHE CHEMIE), Issue 10 2007Wen-Jian Shi Abstract The gold(I)- or Brønsted acid-catalyzed reaction of unactivated vinylcyclopropanes (VCPs) with sulfonamides affords useful homoallylic amine derivatives. This ring-opening reaction occurs in a highly selective manner affording in the case of ,-phenyl-substituted VCPs products with the E -configuration exclusively. [source] Chemistry of some fluorescamine,amine derivatives with relevance to the biosynthesis of benzylpenicillin by fermentationJOURNAL OF CHEMICAL TECHNOLOGY & BIOTECHNOLOGY, Issue 12 2002L Baker Abstract The reaction of fluorescamine with 6-aminopenicillanic acid (6-APA) at pH 4 was investigated for its potential use in the biosynthesis of benzylpenicillin. A number of amino acids and penicillin amine derivatives, that reacted with fluorescamine at pH 7,9, were unlikely to do so to a significant extent at pH 4 and hence were unlikely to interfere in results that led to the biosynthesis of benzylpenicillin. Biosynthesis was followed using Penicillium chrysogenum Wis F3-64, growing in a corn steep liquor medium in a shake flask fed with phenylacetic acid daily. Analysis of benzylpenicillin formation was effected enzymically and fluorimetrically. A sample of the fermentation broth was treated with buffer at pH 7.8 and an active penicillin acylase solution for 1,h at 37,°C. The pH was then lowered to 4 by swamping with acetate buffer and the solution was treated with fluorescamine. The resulting fluorescence was compared with that of a standard 6-aminopenicillianic acid solution treated in the same manner. In this case the biosynthesis of benzylpenicillin was found to increase over 6 days. The results were compared with those for a control broth where the penicillin acylase was not added. © 2002 Society of Chemical Industry [source] Synthesis of [1- 11C]ethyl iodide from [11C]carbon monoxide and its application in alkylation reactionsJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 11 2004Jonas Eriksson Abstract A method is presented for preparing [1- 11C]ethyl iodide from [11C]carbon monoxide. The method utilizes methyl iodide and [11C]carbon monoxide in a palladium-mediated carbonylation reaction to form a mixture of [1- 11C]acetic acid and [1- 11C]methyl acetate. The acetates are reduced to [1- 11C]ethanol and subsequently converted to [1- 11C]ethyl iodide. The synthesis time was 20 min and the decay-corrected radiochemical yield of [1- 11C]ethyl iodide was 55 ± 5%. The position of the label was confirmed by 13C-labelling and 13C-NMR analysis. [1- 11C]Ethyl iodide was used in two model reactions, an O -alkylation and an N -alkylation. Starting with approximately 2.5 GBq of [11C]carbon monoxide, the isolated decay-corrected radiochemical yields for the ester and the amine derivatives were 45 ± 0.5% and 25 ± 2%, respectively, based on [11C]carbon monoxide. Starting with 10 GBq of [11C]carbon monoxide, 0.55 GBq of the labelled ester was isolated within 40 min with a specific radioactivity of 36 GBq/µmol. Copyright © 2004 John Wiley & Sons, Ltd. [source] Design, Synthesis and Evaluation of N -Basic Substituted 3-Hydroxypyridin-4-ones: Orally Active Iron Chelators with Lysosomotrophic PotentialJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 3 2000ZU D. LIU To investigate the possibility of targeting chelators into the lysosomal iron pool, nine bidentate 3-hydroxypyridin-4-ones with basic chains have been synthesized. As the turnover of ferritin iron is centred in the lysosome, such strategy is predicted to increase chelator efficacy of bidentate ligands. The pKa values of the ligands together with their distribution coefficients between 1-octanol and 4-morpholinepropane sulphonic acid (MOPS) buffer pH 7.4 have been determined. The in-vivo iron mobilization efficacy of these basic 3-hydroxypyridin-4-ones has been investigated in a 59Fe-ferritin-loaded rat model. No obvious correlation was observed between efficacy and the pKa value of the side chain, although those with pKa > 7.0 tended to be more efficient than those with pKa < 7.0. The imidazole-containing molecules are much less effective than the tertiary amine derivatives. A dose-response study suggested that basic pyridinones are relatively more effective at lower doses when compared with N -alkyl hydroxypyridinones. Optimal effects were observed with the piperidine derivatives 4h and 4i. The derivative 4i at a dose of 150 ,mol kg,1 was more effective than 450 ,mol kg,1 deferiprone, the widely adopted clinical dose. [source] Aryl acrylate based high-internal-phase emulsions as precursors for reactive monolithic polymer supportsJOURNAL OF POLYMER SCIENCE (IN TWO SECTIONS), Issue 2 2005Peter Krajnc Abstract Water-in-oil high-internal-phase emulsions (HIPEs), containing 4-nitrophenyl acrylate and 2,4,6-trichlorophenyl acrylate as reactive monomers, were prepared and polymerized, and highly porous monolithic materials resulted. The novel materials were studied by combustion analysis, Fourier transform infrared spectroscopy scanning electron microscopy, mercury porosimetry, and N2 adsorption/desorption analysis. With both esters, cellular macroporous monolithic polymers were obtained; the use of 4-nitrophenyl acrylate resulted in a cellular material with void diameters between 3 and 7 ,m and approximately 3-,m interconnects, whereas the use of 2,4,6-trichlorophenyl acrylate yielded a foam with void diameters between 2 and 5 ,m, most interconnects being around 1 ,m. The resulting monoliths proved to be very reactive toward nucleophiles, and possibilities of functionalizing the novel polymer supports were demonstrated via reactions with amines bearing additional functional groups and via the synthesis of an acid chloride derivative. Tris(hydroxymethyl)aminomethane and tris(2-aminoethyl)amine derivatives were obtained. The hydrolysis of 4-nitrophenylacrylate removed the nitrophenyl group, yielding a monolithic acrylic acid polymer. Furthermore, functionalization to immobilized acid chloride was performed very efficiently, with more than 95% of the acid groups reacting. The measurement of the nitrogen content in 4-nitrophenyl acrylate poly(HIPE)s after various times of hydrolysis showed the influence of the total pore volume of the monolithic polymers on the velocity of the reaction, which was faster with the more porous polymer. © 2004 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 43: 296,303, 2005 [source] Stereochemical analysis of N -cyclohexylidene- N -(1-phenylethyl)amine derivativesMAGNETIC RESONANCE IN CHEMISTRY, Issue 12 2005Armando Ariza-Castolo Abstract The configurational properties of a series of cyclohexylidene imines are discussed on the basis of their 1H, 13C and 15N NMR spectral data. Copyright © 2005 John Wiley & Sons, Ltd. [source] | ||||||||||||||||||||||