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Relevant bibliographies by topics / Diazepine

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Academic literature on the topic 'Diazepine'

Author: Grafiati

Published: 4 June 2021

Last updated: 1 February 2022

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Journal articles on the topic "Diazepine"

1

Rashid, Muhammad A., Aisha Ashraf, Sahibzada S. Rehman, Shaukat A. Shahid, Adeel Mahmood, and Muhammad Faruq. "1,4-Diazepines: A Review on Synthesis, Reactions and Biological Significance." Current Organic Synthesis 16, no. 5 (October 17, 2019): 709–29. http://dx.doi.org/10.2174/1570179416666190703113807.

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Background:1,4-Diazepines are two nitrogen containing seven membered heterocyclic compounds and associated with a wide range of biological activities. Due to its medicinal importance, scientists are actively involved in the synthesis, reactions and biological evaluation of 1,4-diazepines since number of decades.Objective:The primary purpose of this review is to discuss the synthetic schemes and reactivity of 1,4- diazepines. This article also describes biological aspects of 1,4-diazepine derivatives, that can be usefully exploited for the pharmaceutical sector.Conclusion:This review summarizes the abundant literature on synthetic routes, chemical reactions and biological attributes of 1,4-diazepine derivatives. We concluded that 1,4-diazepines have significant importance due to their biological activities like antipsychotic, anxiolytic, anthelmintic, anticonvulsant, antibacterial, antifungal and anticancer. 1,4-diazepine derivatives with significant biological activities could be explored for potential use in the pharmaceutical industries.

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Donzello, Maria Pia, Claudio Ercolani, Luisa Mannina, Elisa Viola, Alëna Bubnova, Ol'ga G. Khelevina, and Pavel A. Stuzhin. "Synthesis and Spectroscopic Properties of Low-Symmetry Tribenzoporphyrazines with Annulated 6H-1,4-Diazepine Ring." Australian Journal of Chemistry 61, no. 4 (2008): 262. http://dx.doi.org/10.1071/ch08071.

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Template co-condensation of 2,3-dicyano-5,7-diphenyl-6H-1,4-diazepine 1 with 10-fold molar excess of phthalodinitrile 2 in the presence of MgII propoxide or butoxide in the corresponding alcohol leads to a mixture of MgII-diazepinoporphyrazines 3–6 from which the low symmetry 3:1 species 3, which contains three annulated benzene and one 1,4-diazepine rings, is separated by column chromatography as the aquo complex, [2,4-diphenyltribenzo[b,g,l][1,4]diazepino[2,3-q]porphyrazinato(aquo)magnesium(ii)], [Bz3DzPzMg(H2O)]. The complex 3 can be demetalated in acetic or trifluoroacetic acids under mild conditions with formation of the corresponding free-base [Bz3DzPzH2] 3a. This latter is also formed by co-cyclotetramerization of the same precursors 1 and 2 in the presence of sodium ethoxide in ethanol or lithium butoxide in butanol followed by demetalation of the intermediate disodium or dilithium salts in acid medium. The constitution and structure of the obtained compounds were established on the basis of elemental analysis, mass spectrometry, and 1H NMR spectra. The variable temperature 1H NMR measurements provide evidence that in porphyrazines 3 and 3a the 1,4-diazepine ring exists predominantly in the 6H-form over a wide temperature range. The free energy of activation for the inversion of the 1,4-diazepine ring determined for 3 is 45.6 ± 1.7 kJ mol–1. Solution UV-visible spectra measurements in acidic media (CH2Cl2/CF3COOH) provide evidence that the MgII complex 3 is easily protonated on the meso-N atom of the porphyrazine macrocycle followed by slow demetallation with formation of the free base 3a in its neutral form or as a species protonated on the diazepine ring.

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Zemanová, Ivana, Michaela Potančoková, and Renata Gašparová. "Synthesis of 4-OXO-4H-Chromene Derivative with Fused Benzodiazepine Ring." Nova Biotechnologica et Chimica 15, no. 1 (June 1, 2016): 85–89. http://dx.doi.org/10.1515/nbec-2016-0009.

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Abstract 6-Acetylbenzo[b]chromeno[2,3-e][1,4]diazepin-13(6H)-one 6 was synthesized by reaction of 4- oxo-4H-chromene-3-carboxaldehyde 1 with 1,2-diaminobenzene 2 followed by cyclisation of formed Schiff base 3 and spontaneous oxidation of dihydrodiazepine 4 by air oxygen. Finally, diazepine 5 was acetylated at N(6) by reaction with acetic anhydride.

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Tarakanova, Ekaterina N., Pavel A. Tarakanov, Victor E. Pushkarev, and Larisa G. Tomilova. "The first synthesis of sandwich-type complex based on tetradiazepinoporphyrazine ligand." Journal of Porphyrins and Phthalocyanines 18, no. 01n02 (January 2014): 149–54. http://dx.doi.org/10.1142/s1088424613501113.

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Sandwich-type complex based on tetradiazepinoporphyrazine ligand — bis{tetrakis(5,7-di(4-tert-butylphenyl)-6H-1,4-diazepino)[2,3-b,g,l,q]porphyrazinato}lutetium — was synthesized for the first time. The structure of the compound has been confirmed by UV-vis/NIR, 1 H NMR spectroscopy, and MALDI-TOF mass spectrometry data. The introduction of annulated diazepine heterocycles to porphyrazine molecule significantly changes macrocycle reactivity and results in sandwich-type complex under conditions used for the selective synthesis of lanthanide(III) monophthalocyanines.

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Stuzhin, Pavel A., Pavel Tarakanov, Svetlana Shiryaeva, Anna Zimenkova, Oscar I. Koifman, Elisa Viola, Maria Pia Donzello, and Claudio Ercolani. "Porphyrazines with annulated diazepine rings 4: Synthesis and properties of MgII tetradiazepinoporphyrazine carrying exocyclic styryl fragments." Journal of Porphyrins and Phthalocyanines 16, no. 07n08 (July 2012): 968–76. http://dx.doi.org/10.1142/s1088424612501052.

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A novel tetradiazepinoporphyrazine MgII complex bearing eight peripheral styryl substituents, [St8TDzPAMg(H2O)] ( St = -CH=CHAr , where Ar = 4-methoxyphenyl ) was prepared by template cyclotetramerization of the corresponding precursor — 5,7-distyryl substituted diazepino-2,3-dicarbonitrile — in the presence of MgII butoxide in n-butanol. UV-visible and 1H NMR spectral data indicate that the complex is strongly aggregated in non-coordinating solvents (dichloromethane, chloroform, benzene), it is dimeric in pyridine, whereas it is predominantly monomeric in dimethylsulfoxide and dimethylformamide. The fluorescence response is high for solutions in which the monomeric form is prevalent, but it is strongly quenched as the content of the dimer is increased. Evidence was obtained that dimerization occurs due to intermolecular hydrogen bonding between acidic CH2 groups in the diazepine ring (6H form) of one molecule with meso- and/or diazepine N atoms of another molecule, dimerization being also contributed by the presence of chlatrated water. In the presence of fluoride anions the dimer is destroyed with formation of the monomeric species, which is changed to the 1H form upon heating, as indicated by 1H NMR spectra.

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ANGELONI, SILVIA, and CLAUDIO ERCOLANI. "New classes of porphyrazine macrocycles with annulated heterocyclic rings." Journal of Porphyrins and Phthalocyanines 04, no. 05 (August 2000): 474–83. http://dx.doi.org/10.1002/1099-1409(200008)4:5<474::aid-jpp276>3.0.co;2-w.

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The present contribution summarizes the most recent results on the synthesis and chemical physical characterization of the new classes of porphyrazine macrocycles having annulated five- and seven-membered heterocyclic rings, i.e. tetrakis(thiadizole)porphyrazine, TTDPzH 2, tetrakis(selenodiazole)porphyrazine, TSeDPzH 2, tetrakis-2,3-(5,7dipheny-6H-1,4-diazepino)porphyrazine, Ph 8 DzPzH 2, and a number of their metal derivatives, prepared by using, respectively, 3,4-dicyano-1,2,5-thiadiazole, 3,4-dicyano-1,2,5-selenodiazole, and 5,7-diphenyl-2,3-dicyano-6H-1,4-diazepine as monomeric precursors. The available information indicates that, owing to the presence of electron rich and soft atoms ( S , Se ) inserted in the proximity of the porphyrazine core, the TTDPz and TSeDPz macrocycles, closely resembling their phthalocyanine analogues in terms of structural and electronic features and physical behaviour (solubility, thermal stability, vaporizability, etc.), might be promising new materials for applicative properties. Particularly interesting is the operated peripheral ring opening of the TSeDPz macroxycle leading to the formation of octaaminoporphyrazine, followed by its conversion to a tetrakis(pyrazino)porphyrazine. The macrocycles containing the Ph 8 DzPz skeleton, due to the presence of the external non planar diphenyldiazepine units, appear to exhibit a distinct physical behaviour, which can be probably modulated by appropriate alternative substitutions in the 5, 6, and 7 positions of the diazepine rings.

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Kantlehner, Willi, Jochen Mezger, Hansjörg Lehmann, Kai Edelmann, and Wolfgang Frey. "Orthoamide und Iminiumsalze, XCVa. Umsetzungen von Orthoamiden von Alkin-Carbonsäuren mit Acetophenonen und Acetophenon-Phenylhydrazonen." Zeitschrift für Naturforschung B 73, no. 10 (October 25, 2018): 689–701. http://dx.doi.org/10.1515/znb-2018-0065.

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AbstractThe orthoamides of alkyne carboxylic acids 4 react with acetophenones 5 – catalyzed by trialkylborates – to give ketene aminals 6, which can be transformed to 5-amino-5-hydrazino-penta-2,4-dien-1-ones 10 by treatment with 2,4-dinitro-phenylhydrazine. From acetophenone-phenylhydrazones 12 and orthoamides 4 1H-1,2-diazepines 18 (fett) are formed at room temperature, whereas 4-dimethylamino-pyridines 22 are obtained at elevated temperatures. The diazepine 18a is degraded to the pyridine-derivative 22b upon heating. The N-unsubstituted acetophenone-hydrazone 25 reacts with 4c to give amidrazone 26. The constitution of compounds 18a, 22a, 22b, 26 is established by crystal structure analyses.

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El-Ablack, Fawzia Zakaria. "Synthesis of Some New Benzimidazole Derivatives of Pharmaceutical Interest." E-Journal of Chemistry 8, no. 2 (2011): 748–52. http://dx.doi.org/10.1155/2011/723421.

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Reaction of 2-(aminomethyl)benzimidazole dihydrochloride (1) with ethyl acetoacetate was studied to give diazepinone-benzimidazole derivative (2), while, treatment of 1 with phenylhydrazono ethylacetoacetate afforded phenylhydrazino diazepinone derivative (3). On the other hand, reaction of 1 with acetyl acetone resulted in the formation of diazepine derivative (4). The reaction of 1 with ethyl cyanoacetate was studied to give 3-aminodiazepinone derivative (5). Also the reaction of 1 with acetophenone and/or benzophenone has been investigated to give the fused imidazolines 6 and 7 respectively, while the reaction of 1 with cyclopentanone gave benzimidazolyl derivative (8). Treatment of 1 with chloroacetyl chloride gave the fused pyrazinone (9). The treatment of 1 with benzoin gave the derivative (10). The structures of the hitherto unknown compounds have been confirmed from analytical and spectral data. The newly synthesized compounds were screened for antibacterial and antifungal activity.

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Meszárosová, Kateřina, Antonín Holý, and Milena Masojídková. "Synthesis of Acyclic Adenine 8,N-Anhydronucleosides." Collection of Czechoslovak Chemical Communications 65, no. 7 (2000): 1109–25. http://dx.doi.org/10.1135/cccc20001109.

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9-(4-Hydroxybutyl)adenine (10) was obtained by reaction of adenine with 4-[(2-tetrahydropyran-2-yl)oxy]butyl chloride (7) in the presence of DBU. 8-Bromo-9-(4-hydroxybutyl)adenine (13) was prepared by bromination of 10 or by alkylation of 8-bromoadenine (11) with 4-bromoethyl acetate followed by methanolysis. Tosylation of compound 13 afforded the 4-tosyloxy derivative 15 which gave on heating with methylamine or cyclopropylamine 6-methyl- (17a) or 6-cyclopropyl-7,8,9,10-tetrahydro-6H-[1,3]diazepino[1,2-e]purin-4-amine (17b), while the reaction with hydrazine afforded 7,8,9,10-tetrahydro-6H-[1,3]diazepino[1,2-e]purine-4,6-diamine (17d). Treatment of compound 13 with thionyl chloride gave 9-(4-chlorobutyl)-8-chloroadenine (18) as the main product which was transformed to 17b, 6-propyl-7,8,9,10-tetrahydro-6H-[1,3]diazepino[1,2-e]purin-4-amine (17c) or 7,8,9,10-tetrahydro-6H-[1,3]diazepino[1,2-e]purin-4-amine (17e) by reaction with cyclopropylamine, propylamine or ammonia, respectively. Compound 17e was quite stable both in acid and alkaline solutions, at room temperature or at 90 °C. Compound 13 was converted to 9-(4-hydroxybutyl)-8-methylaminoadenine (19) by reaction with methylamine. Compound 19 failed to undergo intramolecular cyclization to diazepine 17a on treatment with diphenyl carbonate, bis(4-nitrophenyl) carbonate or 1,1'-carbonyldiimidazole.

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Capuano, Ben, Ian T. Crosby, Edward J. Lloyd, Juliette E. Neve, and David A. Taylor. "Aminimides as Potential CNS Acting Agents. I. Design, Synthesis, and Receptor Binding of 4′-Aryl Aminimide Analogues of Clozapine as Prospective Novel Antipsychotics." Australian Journal of Chemistry 60, no. 9 (2007): 673. http://dx.doi.org/10.1071/ch07197.

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A series of substituted 1-[4-(8-chloro-5H-dibenzo[b,e][1,4]diazepin-11-yl)-1-methylhexahydropyrazin-1-ium]-1-aminimide derivatives were designed on the basis of the physicochemical properties of the aminimide functional group and synthesized as potential antipsychotic agents for the treatment of schizophrenia. The target compounds were readily prepared in two steps from clozapine (8-chloro-11-(4-methylpiperazino)-5H-dibenzo[b,e][1,4]diazepine) and involved N-acylation of a common hydrazinium salt intermediate by an acyl chloride or activated ester in the presence of a strong base. The aminimides were tested for in vitro activity at the dopamine D4 and serotonin 5-HT2A receptors and were found to possess modest affinity for both receptor systems.

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Dissertations / Theses on the topic "Diazepine"

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Wilpert, Carsten. "Pyrido[3,2-e][1,4]diazepine : Synthese und Prüfung auf Anti-HIV-1-Wirkung /." [S.l. : s.n.], 1995. http://www.gbv.de/dms/bs/toc/184661447.pdf.

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Raihane, Mohamed. "Reactions d'annelation en serie imidazo(1,2-a)pyridine : acces aux systemes pyridoimidazo(iso)quinoleiniques et imidazopyridodiazepiniques isosteres de tibo." Clermont-Ferrand 1, 1996. http://www.theses.fr/1996CLF1PP01.

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Hamidi, Parinaz. "Design and synthesis of diazepine inhibitors as novel anti-cancer agents." Thesis, Cardiff University, 2006. http://orca.cf.ac.uk/54275/.

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Cancer is a new growth that arises from abnormal and uncontrolled division of cells that may go on to invade and destroy surrounding tissues. The eukaryotic cell cycle consists of a complex sequence of events that regulates cell division and responses to DNA damage. These processes rely upon several key enzymes, including the cyclin dependent kinases (CDKs), checkpoint kinases (Chk2) and poly(ADP-ribose)polymerase-l (PARP-1). CDKs are a family of protein kinases that control progression of the cell cycle, and are themselves regulated by a complex network of activating and inhibitory mechanisms. The vital importance of CDKs in regulating of the cell cycle, emphasise their importance as anti-cancer drug targets. CDKs inhibitors compete with the natural substrate ATP in a competitive manner. Hymenialdisine and kenpaullone have been identified as novel and potent CDK inhibitors both containing an unusual azepinone scaffold. Checkpoint kinase 2 (Chk2) is a novel target for anti-cancer drug design. The enzyme mediates cell proliferation in response to DNA damage by inducing cell cycle arrest, which facilitates the DNA repair pathways. Chk2 inhibition has been recognised as a potential target for the chemopotentiation of current anti-cancer treatments. Few Chk2 inhibitors are known, kenpaullone has been identified as a novel and selective ATP competitive Chk2 inhibitor (IC₅₀ = 0.8 µM). Debromohymenialdisine (DBH) also containing an azepinone scaffold has also been reported to inhibit Chk2. Poly(ADP-ribose)polymerase-l (PARP-1) is activated in response to DNA damage, and inhibition can potentiate cancer chemotherapy and radiotherapy. A PARP-1 inhibitor in combination with a cytotoxic agent should enhance drug activity by blocking the repair capabilities of PARP-1 in cancer cells. Although many types of inhibitors have been identified for each of these three enzymes, compounds containing a seven-membered lactam ring have been identified as key inhibitors for CDKs/Chk2/PARP-l. This study is entered upon developing the synthesis for a series of novel inhibitors of these three enzymes containing the essential lactam pharmacophore in their structures. The compounds synthesised in this study were assessed by a number of biological assays showing moderate or good growth or catalytic inhibitory activity against CDKs and PARP-1 respectively, while assays against Chk2 showed no inhibition.

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Hofmann, Thorsten. "Synthese und Reaktionen von Cyclopenta[c]1,2-diazepinen und Cyclopenta[d]1,2-diazepinen." [S.l.] : [s.n.], 2001. http://deposit.ddb.de/cgi-bin/dokserv?idn=963775774.

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Hamaguchi, Anzu. "Molecular and cellular pharmacology of novel pyrrolo [2,1-c] [1,4] diazepine-based anticancer agents." Thesis, University College London (University of London), 2006. http://discovery.ucl.ac.uk/1444728/.

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The pyrrolo 2,1-c 1,benzodiazepines (PBDs) are a family of naturally occurring antitumour antibiotics which includes anthramycin, DC-81, tomaymycin and sibiromycin. They exert their biological activity through covalent binding to the exocyclic N2 group of guanine in the minor groove of DNA and block transcription in a sequence-specific manner. These PBD monomers span three DNA base pairs and have a preference for binding to purine-G-purine triplets. The PBDs have been used as a scaffold to attach other moieties, leading to novel sequence-selective DNA minor groove alkylating agents. In addition, as part of a rational approach to producing more efficient and selective DNA interstrand crosslinking agents, two PBD monomers have been linked together to form PBD dimers. The research in this thesis is a study of the molecular and cellular pharmacology of several series of novel PBD-containing agents including novel PBD dimers with different linker lengths, PBD-nitrogen mustard conjugates, PBD-polyamide conjugates and C2-aryl PBD monomers. Cytotoxicity in human tumour cell lines, efficiency of DNA interstrand crosslinking in naked linear plasmid DNA, and DNA sequence specificity were assessed. DNA interstrand crosslink formation and repair in cells were also measured. Resulting from this work Q2lQT-exo-unsaturated PBD dimers have been characterised to be highly cytotoxic and efficient in producing interstrand crosslinks both in naked DNA and in cells that are not repaired up to 48 hours. Only two of the PBD-nitrogen mustard conjugates showed some interaction with DNA although several members of this group showed significant cytotoxicity. A PBD-tri-pyrrole conjugate was found to bind preferentially to the sequence 5'-AGATTATC. Novel C2-aryl PBD monomers were shown to bind selectively to 5'-purine-G-purine sequences and demonstrated significant cytotoxicity. In addition, a method utilizing fluorescently end-labelled oligonucleotides was developed and validated to screen libraries of PBD-containing molecules synthesised on beads by combinatorial chemistry. This method allowed the isolation and discrimination of beads containing compounds, which have a high affinity for specific DNA sequences.

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Lourega, Rogério Vescia. "Síntese de 3H-pirido[2,3-b][1,4]diazepinos Trifluormetil Substituídos e Diazepinonas Análogas." Universidade Federal de Santa Maria, 2006. http://repositorio.ufsm.br/handle/1/4143.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
The present research describes new synthetic methodologies for the synthesis of new series of 2-aryl(heteroaryl)-4-trifluoro-4,5-dihydro-3Hpyrido[2,3-b][1,4]diazepin-4-ols and 2-aryl(heteroaryl)-3H-pyrido[2,3-b][1,4]diazepin-4(5H)-one analogs, in a single one-pot procedure or through on intermolecular cyclization reactions of the enaminoketones intermediates, where aryl = Ph, 4-MeC6H4, 4-OMeC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 4,4 -biphenyl, 1-naphtyl and heteroaryl = 2-furyl, 2-thienyl. The pyridodiazepinols were obtained from intramolecular cyclocondensation reactions of enaminoketones N3-[1-aryl(heteroaryl)-3-oxo-4,4,4-trifluorobut-1-en-1-yl]-2,3-diaminopyridines in methanol at temperature of 50 °C for 16 hours. In a one-pot reaction, these pyridodiazepinols can be obtained through reactions of 4-methoxy-1,1,1-trifluorobut-3-en-2-ones with 2,3-diaminopyridine, using methanol as solvent and a temperature of 55 to 60 ºC for 24 hours with yields of 56-68%. The attainment of the 2-aryl(heteroaryl)-3H-pyrido[2,3-b][1,4]diazepin-4(5H)-one analogs were obtained through the haloform intramolecular reactions, with the elimination of the trichloromethyl group, from the synthetic intermediate N3-[1-aryl(heteroaryl)-3-oxo-4,4,4-trichlorobut-1-en-yl]-2,3-diaminopyridines in methanol and a temperature of 65 °C for 20 hours with yield of 48-70%. Therefore, the respective pyridodiazepinones were obatined, in a one-pot reaction, reacting 4-aryl(heteroaryl)-4-methoxy-1,1,1-trichlorobut-3-en-2-ones with 2,3-diaminopyridine in more drastic conditions (methanol, 65 ºC and 24 hours) with yields of 48-70%. Under moderated conditions (methanol, 0 °C and 20 hours), regioselective synthesis between the 4-alkyl(aryl/heteroaryl)-4-methoxy-1,1,1-trihalobut-3-en-2-ones and 2,3-diaminopyridine, leads to the isolation of the respective N3-[1-aryl(heteroaryl)-3-oxo-4,4,4-trihalobut-1-en-1-yl]-2,3-diaminopyridines, through of addition - elimination reactions, in good yields. The N3-[1-aryl-3-oxo-4,4,4-trichlorobut-1-en-1-yl]-N2-[sulphonyl methano]-2,3-diaminopyridines were obtained by sulphonation reaction between the N3-[1-aryl-3-oxo-4,4,4-trichlorobut-1-en-1-yl]-2,3-diaminopyridines and methanesulfonyl chloride, at room temperature for 4 hours with yields of 53-66%. Finally, it was obtained a serie of N 3-[trifluoroacetyl-cycloalken-1-yl]-2,3-diaminopyridines through N-acilation reactions, involving cycloalkanones trifluoromethylated of 5, 7 or 8 members with 2,3-diaminopyridine in methanol at 0 ºC for 20 hours with yields of 65-69%. Subsequent reactions showed that, only under more drastic conditions (methanol, 50 °C e 24 hours), these cyclic enaminones underwent intramolecular cyclization, resulting the pyrido-imidazol as only product, independently of the cycloalkanone precursor. The compounds obtained in this research were identified by 1H and 13C NMR and analyzed by elemental analysis, being the N3-[1-aryl(heteroaryl)-3-oxo-4,4,4-trihalobut-1-en-1-yl]-2,3-diaminopyridines, also identified by X-ray diffraction.
O presente trabalho descreve novas metodologias sintéticas para obtenção de séries inéditas de 2-aril(heteroaril)-4-trifluor-4,5-diidro-3Hpirido[2,3-b][1,4]diazepin-4-óis e 2-aril(heteroaril)-3H-pirido[2,3-b][1,4]diazepin-4(5H)-onas análogas, em passo reacional único ou a partir de reações de ciclização intramoleculares de enaminocetonas intermediárias, sendo aril = Ph, 4-MeC6H4, 4-OMeC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 4,4 -bifenila, 1-naftila e heteroarila = 2-furila, 2-tienila. Os piridodiazepinóis foram obtidos a partir de reações de ciclocondensação intramolecular de enaminocetonas N3-[1-aril(heteroaril)-3-oxo-4,4,4-trifluorbut-1-en-1-il]-2,3-diaminopiridinas em metanol à 50 °C por 16 horas. Enquanto que, em passo reacional único, estes piridodiazepinóis foram obtidos a partir de reações de 4-metoxi-1,1,1-trifluorbut-3-en-2-onas com 2,3-diaminopiridina, utilizando metanol como solvente a uma temperatura de 55 à 60 °C por 24 horas com rendimentos mais satisfatórios que variam entre 56-68%. A obtenção das 2-aril(heteroaril)-3H-pirido[2,3-b][1,4]diazepin-4(5H)-onas análogas foi realizada através das reações de ciclocondensação intramolecular do tipo halofórmica, com eliminação do grupamento triclorometila, partindo dos intermediários sintéticos N3-[1-aril(heteroaril)-3-oxo-4,4,4-triclorobut-1-en-il]-2,3-diaminopiridinas em metanol à temperatura de 65 °C, por 20 horas com rendimentos não satisfatórios. No entanto, as respectivas piridodiazepinonas foram obtidas, em etapa reacional única, reagindo as 4-aril(heteroaril)-4-metoxi-1,1,1-triclorobut-3-en-2-onas com 2,3-diaminopiridina em condições mais drásticas, ou seja, utilizando metanol à temperatura de 65 °C por 24 horas com rendimentos que variam de 48-70%. Sob condições brandas (metanol, 0 °C e 20 horas), a síntese regioseletiva entre as 4-alquil(aril/heteroaril)-4-metoxi-1,1,1-trialobut-3-en-2-onas com 2,3-diaminopiridina, levou ao isolamento das respectivas N3-[1-aril(heteroaril)-3-oxo-4,4,4-trialobut-1-en-1-il]-2,3-diaminopiridinas, através de reações de adiçãoeliminação, com bons rendimentos. As N3-[1-aril-3-oxo-4,4,4-triclorobut-1-en-1-il]-N2-[sulfonil metano]-2,3-diaminopiridinas foram obtidas a partir de reações de sulfonação entre as N3-[1-aril-3-oxo-4,4,4-trialobut-1-en-1-il]-2,3-diaminopiridinas e cloreto de sulfonil metano, utilizando como solvente CH2Cl2 e um tempo reacional de 4 horas, à temperatura de 35 °C com rendimentos que variam de 53-66%. Finalmente, também foi mostrada as reações de ciclização derivadas de uma série de N3-[trifluoracetil-cicloalquen-1-il]-2,3-diaminopiridinas. Estas reações subseqüentes, mostraram que somente sob condições mais drásticas (metanol, 60 °C e 24 h), as enaminonas ciclo-derivadas ciclizam intramolecularmente, resultando como único produto um pirido-imidazol, independentemente da cicloalcanona precursora. Os compostos obtidos nesta tese foram identificados por RMN de 1H e 13C e analisados por análise elementar, sendo os compostos N3-[1-aril(heteroaril)-3-oxo-4,4,4-trialobut-1-en-1-il]-2,3-diaminopiridinas, identificados também por difração de Raios-X.

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Terra, Geovana Garcia. "Síntese, caracterização e ensaios cinéticos de novos complexos com o ligante 6-amino-6-metilperhidro-1,4-diazepina (AAZ)." Florianópolis, SC, 2007. http://repositorio.ufsc.br/xmlui/handle/123456789/90721.

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Dissertação (mestrado) - Universidade Federal de Santa Catarina, Centro de Ciências Físicas e Matemáticas. Programa de Pós-Graduação em Química
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Ligantes N-doadores capazes de se coordenarem facialmente a íons metálicos divalentes são de interesse na síntese de complexos metálicos que mimetizem o ambiente de coordenação de sítios ativos de enzimas que contém resíduos de aminoácidos N-doadores.O ligante AAZ foi utilizado na preparação e caracterização de complexos mononucleares de CuII, ZnII e MnII, e na investigação preliminar da atividade de hidrolase para um complexo de CuII. Os cinco complexos obtidos foram sintetizados e caracterizados por análise de difratometria de raios X, espectroscopia no infravermelho, espectroscopia eletrônica e por ressonância magnética nuclear de H1, eletroquímica e titulação potenciométrica. Observou-se que o AAZ coordenou-se facialmente aos íons metálicos nos complexos 1, 2, 3 e 4, já no complexo 5 o ligante AAZ está coordenado de forma bidentada. Foi também observado nos complexos 1 e 2 a capacidade do AAZ em estabilizar as duas conformações possíveis do efeito Jahn Teller. O estudo eletroquímico do complexo 4 mostrou que o Mn2+ foi estabilizado de forma mais eficiente quando comparado ao complexo [Mn(tacn)2]2+. O ensaio cinético de hidrólise do BNPP com o complexo 5 mostrou um fator de acelereação da hidrólise de 2,1x105 em relação a reação não catalisada. A partir dessas observações, o AAZ apresenta-se como uma excelente opção para a preparação de ligantes de interesse bioinorgânicos.

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Gargadennec-Legouin, Béatrice. "Contribution a l'etude de l'ionisation et de la cinetique d'hydrolyse en milieu aqueux de 1,2,4-triazolo-1,4-diazepines." Rennes 1, 1996. http://www.theses.fr/1996REN10078.

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La these a trait a la determination des constantes d'ionisation et a l'etude de la cinetique d'ouverture d'une thieno-1,2,4-triazolo-1,4-diazepine soluble dans l'eau, appelee conventionnellement nhptt. Les constantes d'ionisation du nhptt et de son produit d'ouverture le nhpto ont ete determinees en milieu aqueux par spectrophotometrie u. V. Et par ph-metrie. Les resultats experimentaux ont ete traites par curve-fitting. Les resultats montrent sans ambiguite que le noyau 1,2,4-triazole possede un caractere basique dans l'eau. Ce point avait echappe aux autres auteurs ayant etudie auparavant ces composes. Quelques unes des valeurs de pka n'ont pu (et ne peuvent) etre assignees en toute certitude a des sites (acido-basiques) bien definis etant donne le probleme des constantes microscopiques. La cinetique d'ouverture reversible du nhptt en nhpto a ete etudiee, en parallele, par polarographie et par spectrophotometrie u. V. . Les constantes sont issues, egalement, du traitement des donnees experimentales par curve fitting. Quelles que soient les conditions experimentales, la cinetique d'ouverture est du premier ordre. Le profil des valeurs des constantes d'ouverture et de fermeture en fonction du ph a ete etabli. Enfin, une relation entre constantes cinetiques apparentes, constantes cinetiques elementaires et constantes d'ionisation a ete etablie. Elle s'avere tres compliquee. Elle fait notamment intervenir les pka macroscopiques et microscopiques, ce qui justifie les etudes precedentes. Elle montre qu'il est impossible d'obtenir les constantes cinetiques elementaires autrement que sous forme de combinaisons lineaires. Les traitements par curve-fitting ont ete realises a l'aide de programmes que nous avons specialement concus suivant les problemes a traiter. Lorsque les domaines de ph l'ont permis, les problemes de force ionique ont ete pris en compte via l'introduction du concept d'activite

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Nascimento, Jedson dos Santos [UNESP]. "Efeitos sedativos e cardiovasculares do midazolam e do diazepam associados ou não à clonidina, em pacientes submetidos a estudos hemodinâmicos por suspeitas de doença arterial coronariana." Universidade Estadual Paulista (UNESP), 2007. http://hdl.handle.net/11449/106013.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
Avaliar a qualidade da sedação e os efeitos sobre a frequencia cardiaca e a pressão arterial do midazolam e do diazepam associados ou nao a clonidina, em pacientes com suspeita de doenca coronariana. Métodos: Foi desenvolvido ensaio clinico prospectivo, duplo cego, randomizado, controlado, com 160 pacientes. Estes apresentavam teste ergometrico ou cintilografia positivos para isquemia miocardica e foram submetidos a cineangiocoronariografias diagnosticas eletivas, divididos em cinco grupos de 32 pacientes cada, de acordo com o farmaco utilizado: grupo C (clonidina 0,5 Êg.kg-1); grupo M (midazolam 40 Êg.kg-1); grupo MC (associacao do midazolam 40 Êg.kg-1 e da clonidina 0,5 Êg.kg-1); grupo D (diazepam 40 Êg.kg-1); grupo DC (associacao do diazepam 40 Êg.kg-1 e da clonidina 0,5 Êg.kg-1). A sedacao foi avaliada com base na escala de Ramsay e no consumo de meperidina (0,04 mg.kg-1) que foi utilizada nos pacientes que apresentaram agitacao ou ansiedade durante o procedimento. A PA invasiva, a FC e o escore de sedacao, foram analisados a cada 5 minutos em 4 diferentes momentos: M1 - inicio do exame; M2 - 5 minutos apos o inicio do exame; M3 - metade do tempo do exame e M4 - final do exame. Resultados: Os grupos foram homogeneos com relacao a PA, FC e sedacao no momento controle (M1). Os pacientes que utilizaram o midazolam apresentaram maiores escores de sedacao e variacao da FC e PA (p<0,05). Os que utilizaram o diazepam ou a clonidina exibiram menores e mais apropriados escores de sedacao para a realizacao do exame e apresentaram menor $ variacao da PA e da FC (p>0,05). A associacao com a clonidina potencializou de forma mais precoce e acentuada os efeitos sedativos do midazolam em relacao ao diazepam (p<0,05). O consumo de meperidina nao diferiu entre os grupos estudados (p>0,10)...
Background to evaluate the effects of midazolam, diazepam and associations with clonidine on heart rate (HR), blood pressure (BP) as well as its sedative effect on patients submitted to coronary angiography. Methods A randomized, controlled and double blind, prospective clinical trial was conducted on 160 patients submitted to an elective coronary angiography. All of them have ergometric test or miocardic cintilography positive to ischemia. They were divided into five groups with 32 patients each: C group (clonidine 0,5 ìg.kg-1); M group (midazolam 40 ìg.kg-1); DC group (midazolam 40 ìg.kg-1 and clonidine 0,5 ìg/kg associated); D group (diazepam 40 ìg/kg); DC group (diazepam 40 ìg/kg and clonidine 0,5 ìg.kg-1 associated). Sedation was evaluated based on the Ramsay Scale. Administration of a 0,04 mg.kg-1 dose of meperidine was given to the patients who were agitated or anxious during the procedure. The invasive BP, HR and sedation score based on Ramsay Scale were analyzed every five minutes and four different intervals were considered for the assessment: M1- at the start of the test; M2 5 minutes after the start of the test; M3 half time of the test; M4 at the end of the test. Results The groups were homogeneous in relation the BP, HR and sedation in the control moment (M1) and there was no difference regarding the weight, age and sex. The patients that used midazolam presented deeper sedation score and HR and BP variability (p<0,05). The patients that used diazepam or clonidine have superficial sedation score and better BP and HR stability. The association with clonidine showed the midazolam sedative effects earlier and $ deeper than diazepam (p<0,05). There was no difference in meperidine use (p>0,10) Conclusions The midazolam presented higher and deeper sedative and cardiovascular effect... (Complete abstract, click eletronic address below)

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Nouvet, André. "Synthèse en solution, en phases liquide et solide de peptidomimétiques contraints à base de perhydro-(1,4)-diazepin-2-ones." Montpellier 2, 1998. http://www.theses.fr/1998MON20111.

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L'utilisation de peptides natifs en tant que medicaments se heurte a des inconvenients inherents a leur metabolisme et a leur manque de specificite. C'est dans le but de resoudre ces problemes que l'axe de recherche concernant les peptidomimetiques contraints a ete developpe. Nous avons synthetise des perhydrodiazepinones dont la structure s'apparente a celle des coudes presents dans certains peptides. Dans ce manuscrit, nous avons decrit differentes voies de synthese dont la principale implique une reaction de mitsunobu afin de realiser l'etape-clef de cyclisation. Cette strategie de synthese a ete adaptee sur supports (polyethylene glycol et resine de wang) dans le but d'obtenir un maximum d'outils utilisables en chimie combinatoire pour construire des librairies de ce type de molecules. Dans la derniere partie, nous avons augmente la diversite moleculaire de la structure en effectuant une synthese a partir d'un pool chiral permettant le controle de la chiralite de l'ensemble des carbones asymetriques.

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Books on the topic "Diazepine"

1

Small, Cathleen. Valium and other antianxiety drugs. New York: Cavendish Square Publishing, 2016.

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Ian, Fryer R., ed. Bicyclic diazepines: Diazepines with an additional ring. New York: Wiley, 1991.

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Fryer, R. Ian. Volume 50, Bicyclic Diazepines: Diazepines with an Additional Ring. Wiley-Interscience, 1991.

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Fryer, R. Ian. Bicyclic Diazepines Vol. 50: Diazepines with an Additional Ring. Wiley & Sons, Incorporated, John, 2009.

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Book chapters on the topic "Diazepine"

1

Watthey, Jeffrey W. H., and James L. Stanton. "Dibenzodiazepines and other Tricyclic Diazepine Systems." In Chemistry of Heterocyclic Compounds: A Series Of Monographs, 1–717. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2008. http://dx.doi.org/10.1002/9780470187227.ch1.

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Weber, K. H. "Neue Entwicklungen auf dem Gebiet der Diazepine." In Nutzen und Gefahren der Therapie mit Benzodiazepinen, 1–14. Heidelberg: Steinkopff, 1987. http://dx.doi.org/10.1007/978-3-642-85358-6_1.

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Fryer, R. Ian, and A. Walser. "Bicyclic 1,2-Diazepines." In Chemistry of Heterocyclic Compounds: A Series Of Monographs, 1–88. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2008. http://dx.doi.org/10.1002/9780470187371.ch1.

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Fryer, R. Ian, and A. Walser. "Bicyclic 1,3-Diazepines." In Chemistry of Heterocyclic Compounds: A Series Of Monographs, 89–182. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2008. http://dx.doi.org/10.1002/9780470187371.ch2.

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Walser, A., and R. Ian Fryer. "Hetero Ring[E][1,4]Diazepines." In Chemistry of Heterocyclic Compounds: A Series Of Monographs, 947–1052. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2008. http://dx.doi.org/10.1002/9780470187371.ch10.

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Fryer, R. Ian, and A. Walser. "[1,4]Diazepines with [B]-Fused Rings." In Chemistry of Heterocyclic Compounds: A Series Of Monographs, 209–427. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2008. http://dx.doi.org/10.1002/9780470187371.ch4.

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Fryer, R. Ian, and A. Walser. "1,4-Diazepines with [A]- or [D]-Fused Rings." In Chemistry of Heterocyclic Compounds: A Series Of Monographs, 183–207. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2008. http://dx.doi.org/10.1002/9780470187371.ch3.

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Iden, Hassan S., and William D. Lubell. "Solid-Phase Synthesis of 1,3,5-Trisubstituted 1,4-Diazepin-2-one Peptide Mimic." In Advances in Experimental Medicine and Biology, 213–14. New York, NY: Springer New York, 2009. http://dx.doi.org/10.1007/978-0-387-73657-0_98.

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Deaudelin, Philippe, and William D. Lubell. "Synthesis of pyrrolo[3,2-e][1,4]diazepin-2-ones as potential γ-turn mimetics." In Advances in Experimental Medicine and Biology, 183–84. New York, NY: Springer New York, 2009. http://dx.doi.org/10.1007/978-0-387-73657-0_84.

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Ohta, Yusuke. "Concise Synthesis of Indole-Fused 1,4-Diazepines through Copper(I)-Catalyzed Domino Three-Component Coupling-Cyclization-N-Arylation under Microwave Irradiation." In Copper-Catalyzed Multi-Component Reactions, 63–75. Berlin, Heidelberg: Springer Berlin Heidelberg, 2011. http://dx.doi.org/10.1007/978-3-642-15473-7_4.

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Conference papers on the topic "Diazepine"

1

Hosmane, Ramachandra, and Huanming Chen. "Synthesis of Novel Acyclic Nucleoside and Acyclic Nucleoside Phosphonate Analogues of a Ring-Expanded ("Fat") Nucleobase Containing the Imidazo[4,5-e][1,3]diazepine Ring System." In The 3rd International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 1999. http://dx.doi.org/10.3390/ecsoc-3-01745.

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Sanz, Dionisia, Ana Andrade, Rosa M. Claramunt, and José Elguero. "Synthesis and Structural Characterization of 1,4-Diazepines Related to Curcumin." In The 19th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2015. http://dx.doi.org/10.3390/ecsoc-19-a044.

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Shutalev, Anatoly, and Anastasia Fesenko. "Ring Expansion Tetrahydropyrimidin-2-ones into Tetrahydro-1H-1,3-diazepin-2-ones: a Theoretical Study." In The 21st International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2017. http://dx.doi.org/10.3390/ecsoc-21-04766.

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Shutalev, Anatoly, and Anastasia Fesenko. "Diastereoselectivity in the Ring Expansion of Tetrahydropyrimidin-2-ones into Tetrahydro-1H-1,3-diazepin-2-ones." In The 19th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2015. http://dx.doi.org/10.3390/ecsoc-19-a034.

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