Relevant bibliographies by topics / Imidazo [4

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Academic literature on the topic 'Imidazo [4'

Author: Grafiati
Published: 4 June 2021
Last updated: 14 February 2022

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Journal articles on the topic "Imidazo [4"

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Zhou, Qifan, Fangyu Du, Yajie Shi, Ting Fang, and Guoliang Chen. "Synthesis and Analysis of 1-Methyl-4-Phenyl-1H-Imidazol-2-Amine." Journal of Chemical Research 42, no. 12 (2018): 608–10. http://dx.doi.org/10.3184/174751918x15414286606248.

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A practical synthetic route to an important pharmaceutical intermediate 1-methyl-4-phenyl-1H-imidazol-2-amine, via a three-step sequence involving cyclisation, hydrolysis and methylation, is reported. In the process of optimisation, a novel chemical entity was isolated and confirmed to be 2,6-diphenyl-1H-imidazo[1,2-a]imidazole by MS, 1H NMR and 13C NMR. The scale-up experiment was carried out to provide 1-methyl-4-phenyl-1H-imidazol-2-amine in 27.4% total yield.
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Balewski, Łukasz, Franciszek Sączewski, Patrick J. Bednarski, et al. "Synthesis, Structure and Cytotoxicity Testing of Novel 7-(4,5-Dihydro-1H-imidazol-2-yl)-2-aryl-6,7-dihydro-2H-imidazo[2,1-c][1,2,4]triazol-3(5H)-Imine Derivatives." Molecules 25, no. 24 (2020): 5924. http://dx.doi.org/10.3390/molecules25245924.

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The appropriate 1-arylhydrazinecarbonitriles 1a–c are subjected to the reaction with 2-chloro-4,5-dihydro-1H-imidazole (2), yielding 7-(4,5-dihydro-1H-imidazol-2-yl)-2-aryl-6,7-dihydro-2H-imidazo[2,1-c][1,2,4]triazol-3(5H)-imines 3a–c, which are subsequently converted into the corresponding amides 4a–e, 8a–c, sulfonamides 5a–n, 9, ureas 6a–I, and thioureas 7a–d. The structures of the newly prepared derivatives 3a–c, 4a–e, 5a–n, 6a–i, 7a–d, 8a–c, and 9 are confirmed by IR, NMR spectroscopic data, as well as single-crystal X-ray analyses of 5e and 8c. The in vitro cytotoxic potency of these compounds is determined on a panel of human cancer cell lines, and the relationships between structure and antitumor activity are discussed. The most active 4-chloro-N-(2-(4-chlorophenyl)-7-(4,5-dihydro-1H-imidazol-2-yl)-6,7-dihydro-2H-imidazo[2,1-c][1,2,4]triazol-3(5H)-ylidene)benzamide (4e) and N-(7-(4,5-dihydro-1H-imidazol-2-yl)-2-(p-tolyl)-6,7-dihydro-2H-imidazo[2,1-c][1,2,4]triazol-3(5H)-ylidene)-[1,1′-biphenyl]-4-sulfonamide (5l) inhibits the growth of the cervical cancer SISO and bladder cancer RT-112 cell lines with IC50 values in the range of 2.38–3.77 μM. Moreover, N-(7-(4,5-dihydro-1H-imidazol-2-yl)-2-phenyl-6,7-dihydro-2H-imidazo[2,1-c][1,2,4]triazol-3(5H)-ylidene)-4-phenoxybenzenesulfonamide (5m) has the best selectivity towards the SISO cell line and induces apoptosis in this cell line.
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Demchenko, Sergii, Roman Lesyk, Oleh Yadlovskyi, et al. "Synthesis, Antibacterial and Antifungal Activity of New 3-Aryl-5H-pyrrolo[1,2-a]imidazole and 5H-Imidazo[1,2-a]azepine Quaternary Salts." Molecules 26, no. 14 (2021): 4253. http://dx.doi.org/10.3390/molecules26144253.

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A series of novel 3-aryl-5H-pyrrolo[1,2-a]imidazole and 5H-imidazo[1,2-a]azepine quaternary salts were synthesized in 58–85% yields via the reaction of 3-aryl-6, 7-dihydro-5H-pyrrolo[1,2-a]imidazoles or 3-aryl-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepines and various alkylating reagents. All compounds were characterized by 1H NMR, 13C NMR, and LC-MS. The conducted screening studies of the in vitro antimicrobial activity of the new quaternary salts derivatives established that 15 of the 18 newly synthesized compounds show antibacterial and antifungal activity. Synthesized 3-(3,4-dichlorohenyl)-1-[(4-phenoxyphenylcarbamoyl)-methyl]-6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-1-ium chloride 6c possessed a broad activity spectrum towards Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, and Cryptococcus neoformans, with a high hemolytic activity against human red blood cells and cytotoxicity against HEK-293. However, compound 6c is characterized by a low in vivo toxicity in mice (LD50 > 2000 mg/kg).
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Prasad, Pratibha, Anirudhdha G. Kalola, and Manish P. Patel. "Microwave assisted one-pot synthetic route to imidazo[1,2-a]pyrimidine derivatives of imidazo/triazole clubbed pyrazole and their pharmacological screening." New Journal of Chemistry 42, no. 15 (2018): 12666–76. http://dx.doi.org/10.1039/c8nj00670a.

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An efficient synthetic microwave-assisted, one-pot three-component condensation route for imidazo[1,2-a]pyrimidine derivatives of imidazole 4/triazole 5 clubbed pyrazole catalysed by ecofriendly base KOH.
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Rahimizadeh, Mohammad, Mehdi Pordel, Mehdi Bakavoli, Shima Rezaeian, and Hossein Eshghi. "Synthesis of a new heterocyclic system — Fluoreno[1,2-d]imidazol-10-one." Canadian Journal of Chemistry 87, no. 6 (2009): 724–28. http://dx.doi.org/10.1139/v09-062.

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Synthesis of various substituted fluoreno[1,2-d]imidazol-10-ones (5a–5g) has been accomplished by the cyclization of diazotized 1-substituted 4-benzoyl-5- aminobenzimidazoles (4a–4g). Compounds 4a–4g were prepared by reductive ring opening of 3H-imidazo[4′,5′:3,4]benzo[c]isoxazoles (3a–3g) with zinc dust in EtOH/NaOH solution.
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Loubidi, M., C. Pillard, A. El Hakmaoui, P. Bernard, M. Akssira, and G. Guillaumet. "A new synthetic approach to the imidazo[1,5-a]imidazole-2-one scaffold and effective functionalization through Suzuki–Miyaura cross coupling reactions." RSC Advances 6, no. 9 (2016): 7229–38. http://dx.doi.org/10.1039/c5ra25520a.

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A pathway to new 7-bromo-1-(4-methoxybenzyl)-5-methyl-imidazo[1,5-a]imidazole-2-one was reported. The synthetic potential of this scaffold was demonstrated by displacing bromine by Suzuki–Miyaura cross-coupling reactions.
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Jaberi, Hamid Reza, and Hadi Noorizadeh. "Synthesis of Some Novel Fused Imidazo [2, 1-b] [1, 3] Thiazole and Imidazo [2, 1-b] Thiazolo [5, 4-d] Isoxazole Derivatives." E-Journal of Chemistry 9, no. 3 (2012): 1518–25. http://dx.doi.org/10.1155/2012/896454.

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In this work we describe the synthesis of some novel fused imidazo [2, 1-b] [1, 3] thiazole derivatives. The reaction of 1, 2-diaminoethane 1 with carbon disulphide in H2O/ETOH as solvent furnishes 4, 5-dihydro-1H-imidazol-2-thiol 2 under reflux condition. the reaction of 4,5-dihydro-1H-imidazol-2-thiol on treatment with ethylchloro acetate and aromatic aldehyde in presence of anhydrous sodium acetate and acetic acid as solvent to give (Z)-2-(arylidene)-5,6-dihydroimidazo [2,1-b] [1,3] thiazol-3(2H)-one 3a-j. Compounds 3a-j was condensed with hydroxylamine to give 3-(aryl)-2, 3, 6, 7-tetrahydroimidazo [2, 1-b] [1,3] thiazolo [5, 4-d] isoxazole 4a-j. The structures of the new compounds were established by elemental analyses, IR,1H NMR and13C NMR data.
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Abdulaeva, Inna A., Kirill P. Birin, Yulia G. Gorbunova, Aslan Yu Tsivadze, and Alla Bessmertnykh-Lemeune. "Post-synthetic methods for functionalization of imidazole-fused porphyrins." Journal of Porphyrins and Phthalocyanines 22, no. 08 (2018): 619–31. http://dx.doi.org/10.1142/s1088424618500475.

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Several methods for the post-synthetic modification of imidazo[4,5-[Formula: see text]]porphyrins are reported. First, a synthetic approach to the isomeric difunctionalized porphyrins, containing two [Formula: see text]-fused 2-aryl-1[Formula: see text]-imidazole cycles at adjacent or opposite pyrrole rings of the macrocycle is developed. The core chemistry of this synthetic route is the transformation of 2-aryl-1[Formula: see text]-imidazo[4,5-[Formula: see text]]porphyrins into corresponding imidazodioxochlorins followed by Debus–Radziszewski condensation with aromatic aldehyde. Next, 2-(4-bromophenyl)-1[Formula: see text]-imidazo[4,5-[Formula: see text]]-5,10,15,20-tetramesitylporphyrin was transformed into useful carboxy- and phosphonato-substituted precursors for material chemistry according to palladium-catalyzed C–C and C–P bond forming reactions.
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Bunev, Alexander S., Elena V. Sukhonosova, Vladimir E. Statsyuk, Gennady I. Ostapenko, and Victor N. Khrustalev. "6-(4-Chlorophenyl)-3-methylimidazo[2,1-b]thiazole." Acta Crystallographica Section E Structure Reports Online 69, no. 11 (2013): o1701. http://dx.doi.org/10.1107/s1600536813028833.

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In the title compound, C12H9ClN2S, the imidazo[2,1-b]thiazole fragment is planar (r.m.s. deviation = 0.003 Å), and the benzene ring is twisted slightly [by 5.65 (6)°] relative to this moiety. In the crystal, molecules are linked by π–π stacking interactions into columns along [010]. The molecules within the columns are arranged alternatively by their planar rotation of 180°. Thus, in the columns, there are the two types of π–π stacking interactions, namely, (i) between two imidazo[2,1-b]thiazole fragments [interplanar distance = 3.351 (2) Å] and (ii) between an imidazo[2,1-b]thiazole fragment and the phenyl ring [interplanar distance = 3.410 (5) Å]. There are no short contacts between the columns.
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Bourichi, Selma, Youssef Kandri Rodi, Tuncer Hökelek, Amal Haoudi, Catherine Renard, and Frédéric Capet. "Crystal structure and Hirshfeld surface analysis of 4-allyl-6-bromo-2-(4-chlorophenyl)-4H-imidazo[4,5-b]pyridine." Acta Crystallographica Section E Crystallographic Communications 75, no. 1 (2019): 43–48. http://dx.doi.org/10.1107/s2056989018017322.

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The title compound, C15H11BrClN3, is built up from a planar imidazo[4,5-b]pyridine unit linked to phenyl and allyl substituents. The allyl substituent is rotated significantly out of the imidazo[4,5-b]pyridine plane, while the benzene ring is inclined by 3.84 (6)° to the ring system. In the crystal, molecules are linked via a pair of weak intermolecular C—H...N hydrogen bonds, forming an inversion dimer with an R 2 2(20) ring motif. The dimers are further connected by π–π stacking interactions between the imidazo[4,5-b]pyridine ring systems [centroid–centroid distances = 3.7161 (13) and 3.8478 (13) Å]. The important contributions to the Hirshfeld surface are H...H (35.9%), H...Cl/Cl...H (15.0%), H...C/C...H (12.4%), H...Br/Br...H (10.8%), H...N/N...H (7.5%), C...Br/Br...C (5.9%), C...C (5.5%) and C...N/N...C (4.0%) contacts.
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Dissertations / Theses on the topic "Imidazo [4"

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Arico, Joseph William. "3-Substituted Purines: Methodology, Synthesis, and Studies of DNA Hydration in the Minor Groove." Thesis, Boston College, 2010. http://hdl.handle.net/2345/1824.

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Thesis advisor: Mary F. Roberts<br>As the central repository of biological information and ultimate mediator of all processes underlying the activities of living organisms, nucleic acids are the sine qua non for life as we know it. Biological research over the past century and more has revealed much of the structure and function of nucleic acids, revealing in turn how life begins, changes, reproduces, and ends. We glimpse how life has become what it is and perhaps what it may become. This work seeks to understand the ramifications of altering a single nitrogen of the purine nucleoside components of nucleic acids. As will be shown, purine analogs lacking the N3 nitrogen have altered interactions with proteins, water, and other molecules. Replacement of this nitrogen with a C-H, C-CH3, or C-CH2OH functionality impacts the structure and biological interactions of a DNA duplex containing these alterations in ways not entirely foreseen when this work began over ten years ago. The synthetic effort needed to obtain purine nucleosides containing each of these modifications is significant. Along the way, new methodologies applicable both to the synthesis of purine analogs and natural purine nucleosides are described<br>Thesis (PhD) — Boston College, 2010<br>Submitted to: Boston College. Graduate School of Arts and Sciences<br>Discipline: Chemistry
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Copin, Chloé. "Exploration moléculaire en série imidazo[2, 1-b][1, 3, 4]thiadiazole : applications à la synthèse d'inhibiteurs de kinases impliqués dans les maladies neurodégénératives." Thesis, Orléans, 2013. http://www.theses.fr/2013ORLE2074.

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Depuis plus d’un siècle, la chimie hétérocyclique représente l’un des plus vastes domaines de recherche en chimie organique. En particulier, les hétérocycles bicycliques fusionnés à 5 chaînons, contenant à la fois des atomes de soufre et d’azote, présentent, de par leur rareté et leur potentiel biologique, un champ d’intérêt croissant pour les équipes de recherche et développement académiques ou des entreprises pharmaceutiques. Parmi les nombreux composés bicycliques [5-5], notre étude s’est focalisée sur le noyau imidazo[2,1-b][1,3,4]thiadiazole décrit sporadiquement dans la littérature et pour lequel les voies d’accès actuelles ne se limitent qu’à une seule méthode faisant intervenir une étape de cyclisation et des conditions drastiques. Ce verrou entraine inéluctablement une faible diversité fonctionnelle autour de cet hétérocycle, restreignant ainsi les domaines d’applications notamment biologiques. Afin de pallier à cette problématique, nous avons initié une étude de la réactivité de chacune des trois positions fonctionnalisables du bicycle imidazo[2,1-b][1,3,4]thiadiazole, développant ainsi diverses réactions pallado-catalysées (Suzuki-Miyaura, CH-arylation, Buchwald-Hartwig), de substitution nucléophile aromatique et de Pictet-Spengler. L’étude des propriétés biologiques des différents composés synthétisés et hautement valorisables durant ces travaux a abouti à la découverte de deux séries de molécules inhibant sélectivement les kinases DYRK-1A et CLK-1, deux protéines d’intérêt dans le traitement des affections du système nerveux central (neuropathies, Alzheimer…)<br>For more than a century, heterocyclic chemistry is one of the largest area in organic chemistry research. In particular, because of their rarity and their biological potential, [5-5] fused ring heterocycles containing both sulfur and nitrogen atoms are a large area of interest for both academic and industrial research and development teams. Among these numerous [5-5] bicycles, our study is focused on imidazo[2,1-b][1,3,4]thiadiazole scaffold, which is quite few described in the literature and whose pathways are limited to almost one method involving a cyclisation step and drastic conditions. This lock leads inevitably to low functional diversity around this heterocycle, thus restricting its applications, including biological. In order to overcome this problematic, we then initiated the reactivity study of each three positions of the bicycle imidazo[2,1-b][1,3,4]thiadiazole, developing thereby several palladium couplings (Suzuki-Miyaura, direct arylation, Buchwald-Hartwig), as well as aromatic nucleophilic substitution and Pictet-Spengler reaction. The study of the biological properties of the different compounds synthesized in this work and highly valuable led to the discovery of two series of molecules, inhibiting selectively DYRK-1A and CLK-1, two kinases of interest in the treatment of dysfunction of central nervous system (neuropathies, Alzheimer…)
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Hallé, François. "Conception, développement et synthèse de ligands du TSPO dans le but de traiter les maladies neurodégénératives." Thesis, Strasbourg, 2015. http://www.theses.fr/2015STRAF054/document.

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Les neurostéroïdes sont des composés endogènes qui peuvent moduler la transmission synaptique et avoir un effet neuroprotecteur dans les maladies neurodégénératives. Les systèmes régulant leur biosynthèse ne sont pas connus mais la première étape de celle-ci peut être régulée par la protéine TSPO. Cette protéine mitochondriale facilite le transport du cholestérol vers l’intérieur de la mitochondrie pour y être métabolisé en prégnénolone. Ce stéroïde est le précurseur principal de la biosynthèse des neurostéroïdes et l’utilisation in vitro de ligands du TSPO permet d’augmenter sa sécrétion. Dans ce travail de thèse, nous avons ainsi cherché à développer de nouvelles familles de ligands solubles du TSPO augmentant la sécrétion de prégnénolone. Le développement de ces nouvelles familles a nécessité la réalisation d’une méthodologie de synthèse faisant intervenir une réaction de cyclisation pallado-catalysée de type Buchwald-Hartwig. Une étude de solubilité des composés synthétisés a été effectuée expérimentalement, leur activité a été évaluée par des méthodes fonctionnelles et leur effet neuroprotecteur a été testé sur un modèle cellulaire de la maladie d’Alzheimer<br>Neurosteroids are endogenous compounds which can alter the synaptic transmission and enhance neuroprotection in neurodegenerative diseases. The systems that regulates their biosynthesis are not described but its first step ca be regulated by the TSPO. This mitochondrial protein facilitates the transport of cholesterol to the mitochondrial matrix to be metabolized in pregnenolone. This steroid is the precursor of neurosteroid biosynthesis and in vitro use of TSPO ligands induces its secretion. For this project, we looked forward to develop new families of soluble TSPO ligands that can increase pregnenolone production. The access to 3-amino-3,4-dihydroquinolin-2-ones required the establishment of a synthesis methodology of a palladium-catalyzed cyclization following Buchwald-Hartwig amination. A solubility study of synthesized compound was performed, their activity was established based on functional assays and their neuroprotective effect was evaluated on a cellular model of Alzheimer disease
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Zeinyeh, Waël. "Conception et synthèse d'hétérocycles azotés et de dérivés stéroïdiens, modulateurs potentiels de transporteurs ABC (glycoprotéine-P)." Phd thesis, Université Claude Bernard - Lyon I, 2010. http://tel.archives-ouvertes.fr/tel-00874305.

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La multichimiorésistance est caractérisée par une résistance simultanée à des agents chimiothérapeutiques de structures diverses, induite notamment par l'efflux des substances actives hors des cellules. Les transporteurs ABC (ATP-Binding Cassette) sont des protéines transmembranaires impliquées dans cet efflux et qui participent à l'échec du traitement de certains cancers. Par ailleurs, ce mécanisme d'efflux a également été évoqué dans le cadre de la résistance de certains microorganismes aux antimicrobiens. Dans cette étude, nous avons conçu et synthétisé des dérivés susceptibles d'inhiber certains transporteurs ABC, en particulier, la glycoprotéine-P (Pgp) impliquée dans la multichimiorésistance des tumeurs humaines, et CpABC3, rencontré chez le parasite Cryptosporidium parvum. Dans un premier temps, nous avons synthétisé trois dérivés de type 4-alkyl-imidazo[4,5-b]pyridin-7-one, hétérocycles destinés à se fixer sur le site à ATP des transporteurs ABC. L'activité de ces composés a été évaluée vis-à-vis d'un fragment recombinant (H6-NBD1) de CpABC3, et un de ceux-ci a montré une liaison (faible) à ce fragment. Nous avons ensuite préparé dix-sept dérivés bivalents susceptibles d'inhiber la Pgp, constitués d'une molécule d'adénine (ciblant le site à ATP) reliée à la progestérone (ciblant le site aux stéroïdes) par un bras de géométrie variable. Ces dérivés ont été testés sur des lignées cellulaires K562/R7 surexprimant la Pgp, et un de ceux-ci a montré une activité supérieure à celle de la progestérone. Enfin, nous avons mis au point une synthèse de chaînes de type oligocyclohexylidène, qui sont de bons candidats pour constituer des bras espaceurs rigides
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Ta, Hue Thu. "Reactions of 5-(3-alkyltriazeno)imidazole-4-carboxamide." Thesis, University of Newcastle Upon Tyne, 1990. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.315657.

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Campos, Fátima de. "Síntese e atividade biológica de imidas derivadas da 4-Aminoantipirina." Florianópolis, SC, 2001. http://repositorio.ufsc.br/xmlui/handle/123456789/81474.

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Dissertação (mestrado) - Universidade Federal de Santa Catarina, Centro de Ciências Físicas e Matemáticas. Programa de Pós-Graduação em Química.<br>Made available in DSpace on 2012-10-19T04:25:45Z (GMT). No. of bitstreams: 0Bitstream added on 2014-09-25T19:52:47Z : No. of bitstreams: 1 181665.pdf: 4463435 bytes, checksum: cf584d1d881317feaa6ab54b96a69ece (MD5)<br>Síntese de novas imidas obtidas através da reação entre a 4-aminoantipirina e diferentes anidridos e avaliação da atividade biológica. O composto mais promissor foi selecionado e diferentes modificações estruturais foram realizadas. Os compostos foram obtidos em moderados a excelentes rendimentos (40-95%) e suas estruturas foram confirmadas por dados espectroscópicos (IV e RMN).
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Thiverny, Maryse. "1-oxy-2,3-dihydro-imidazol-4-ones : des intermédiaires et des cibles." Université Joseph Fourier (Grenoble), 2010. http://www.theses.fr/2010GRE10174.

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Les travaux présentés s'articulent autour de synthons nitrone de type N-oxy-imidazolidinone, pour lesquels nous avons exploré les applications possibles. Nous avons développé une nitrone achirale, CYCNO, accessible en 3 étapes depuis un ester de la glycine (66%) et une nitrone chirale, MiPNO. Celle-ci a été obtenue sous forme énantiopure par une méthode de résolution nouvelle ; chaque énantiomère est ainsi accessible avec des rendements de 15 et 17% depuis l'ester de la glycine. CYCNO a été utilisée comme modèle pour étudier la réactivité des N-oxy-imidazolidinones vis-à-vis des halogénures d'aryl- et hétéroarylmagnésium, préparés par insertion de magnésium ou par échange iode-magnésium. La réoxydation des hydroxylamines intermédiaires mène à une nouvelle série de nitrones, pouvant être utilisées comme pièges à radicaux libres. MiPNO a été utilisée pour la préparation d'acides aminés non naturels, arylglycines et α-aryl,α-méthylglycines. La séquence met en jeu une réaction d'addition d'organomagnésiens totalement diastéréosélective. Sept cibles arylglycines ont été préparées. De plus, des réactions de cycloaddition 1,3-dipolaire entre MiPNO et différents alcènes ont conduit à des isoxazolidines, obtenues de façon hautement régio- et diastéréosélective. Le cycloadduit peut être converti en l'α-amino-γ-lactone correspondante en une seule opération, ce qui a mené à la préparation d'un nouveau γ-hydroxy-α-amino-acide énantiopur<br>The present work deals with N-oxy-imidazolidinone type nitrones and the possible applications thereof. We developed an achiral nitrone, CYCNO, available in 3 stages from a glycine ester (66%) and a chiral nitrone, MiPNO. The latter was obtained in enantiopure form by a new optical resolution method; each enantiomer is accessible in 15 and 17% yield from the glycine ester. CYCNO was used as a model to study the reactivity of N-oxy-imidazolidinones toward aryl and heteroarylmagnesium halides, prepared by magnesium insertion or iodine-magnesium exchange. The reoxidation of the intermediate hydroxylamine led to a new family of nitrones, which may be used as spin traps. MiPNO was used for the preparation of unnatural amino acids, arylglycines and α-aryl,α-methylglycines. The sequence involves a totally diastereoselective addition of organomagnesium reagents. Seven arylglycine targets were prepared. In addition, 1,3-dipolar cycloaddition reactions between MiPNO and various alkenes led to isoxazolidines, in excellent regio- and diastereoselectivity. The cycloadduct can be converted into the corresponding α-amino-γ-lactone in a single operation, allowing the preparation of a new enantiopure γ-hydroxy-α-amino-acid
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Kerscher-Hack, Silke [Verfasser]. "Synthese potentieller GABA-uptake-Inhibitoren mit 1H-Imidazol-4-ylessigsäure- und 3-(1H-Imidazol-2-yl)propansäure-Grundstruktur / Silke Gabriele Hack." München : Verlag Dr. Hut, 2011. http://d-nb.info/1014848482/34.

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Boukraa, Sadok. "Préparation, réactivité et étude des propriétés fongistatiques et immunostimulantes d'amino-2 thiazoles et d'imidazo-(2,1-B) thiazoles." Besançon, 1987. http://www.theses.fr/1987BESA2030.

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Le travail se divise en deux grandes parties : la premiere concerne la preparation d'aryl-6 imidazo(2,1-b) thiazoles substitues en 3 par des chaines de type acetate d'ethyle, aroylmethyle. (beta -hydroxy beta -aryl)ethyle te arylethyle. Pour ce faire, il a ete necessaire de preparer les amino-2 thiazoles corespondants substitues par ces memes chaines en 4 afin de las opposer a des acetophenones omega -bromees. L'influence des substituants presents est discutee en vue d'aprehender l'evolution des reactions. La seconde partie concerne des essais en tant que fongistatiques et/ou immunostimulants des composes preparees. Il ressort que les aminothiazoles sont plus interessants que les imidazothiazoles auusi bien sur l'inhibition de croissance de mycelium (epidermophyton) ou de germination des spores (candida, aspergillus) que sur la stimulation du lymphocyte t humain
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NASCIMENTO, André Augusto Pimentel Liesen. "Síntese e avaliação de atividades Anti-Toxoplama gondii e antimicrobiana de Tiossemicarbazidas, 4- Tiazolidinonas e 1,3,4-Tiadiazóis obidos a partir do Éster 5-Metil-1H-Imidazol-4-Carboxilato de Etila." Universidade Federal de Pernambuco, 2007. https://repositorio.ufpe.br/handle/123456789/3514.

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Made available in DSpace on 2014-06-12T16:31:38Z (GMT). No. of bitstreams: 2 arquivo6183_1.pdf: 1683765 bytes, checksum: b5847d9d54b73793b7e809056f871fd5 (MD5) license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) Previous issue date: 2007<br>Doenças parasitárias, como a toxoplasmose, afetam milhões de pessoas no mundo inteiro e são amplamente pesquisadas. Este fato deve-se, em parte, à elevada disseminação dessas doenças em pacientes imunocomprometidos, principalmente naqueles que apresentam a síndrome da imunodeficiência adquirida (AIDS). A toxoplasmose é uma infecção causada por Toxoplasma gondii, parasita com biologia bastante complexa e de caráter cosmopolita, estando largamente distribuído nas diversas áreas geográficas do globo terrestre. Em trabalho publicado recentemente por nosso grupo de pesquisa, foi observado que tiossemicarbazonas e aril-hidrazono-4-tiazolidinonas, substituídas na porção aril com grupo nitro, possuem notória atividade anti-T. gondii. Nos últimos anos, várias publicações têm abordado compostos contendo o núcleo imidazol como potenciais agentes antiprotozoários. Principalmente para análogos do megazol (2-amino-5-(1-metil-5-nitro-2- imidazolil)-1,3,4-tiadiazol) atuando como agentes antichagásicos. Com o objetivo de produzir novas moléculas ativas contra T. gondii desenvolvemos a síntese e avaliação in vitro para aciltiossemicarbazidas (e seus derivados: 4- tiazolidinonas e 1,3,4-tiadiazóis) obtidas a partir do éster etil(5-metil-1-Himidazol- 4-carboxilato). Aciltiossemicarbazidas foram sintetizadas através da reação de adição entre 5-metil-1H-imidazol-4-carboidrazida e isotiocianatos substituídos. A partir destas, foram obtidas duas novas séries: 4-tiazolidinonas, através de uma reação tia-Michael envolvendo anidrido maléico como aceptor de Michael; e 1,3,4-tiadiazóis por uma ciclodesidratação com ácido sulfúrico. Os produtos finais foram purificados por recristalizações (tiossemicarbazidas) e cromatografia em coluna (4-tiazolidinonas) em solventes apropriados, obtendose rendimentos entre 10% e 94%, e caracterizados estruturalmente por métodos espectroscópicos convencionais (RMN 1H, RMN 13C, IV) e espectrometria de massas de alta resolução (MS-HR). A formação de aciltiossemicarbazidas foi confirmada principalmente em RMN 13C, onde sinais em 181,1-181,0 ppm e 163,1-162,5 ppm evidenciaram os grupos C=S e C=O, respectivamente. Para 4-tiazolidinonas, bandas de absorção encontradas entre 1397-1378 cm-1, referentes à deformação angular do grupo NCS, confirmaram o fechamento do anel. Os derivados 1,3,4-tiadiazóis foram caracterizados observando-se a ausência de sinais entre 181,1-181,0 ppm e 163,1-162,5 ppm em espectros de RMN 13C referentes aos grupos C=S e C=O. A existência de troca química em aciltiossemicarbazidas, envolvendo átomos de H lábeis, foi confirmada através da análise espectroscópica de troca química (EXSY). Os resultados de atividade anti-T. gondii indicaram as aciltiossemicarbazidas e os derivados contendo o núcleo 1,3,4-tiadiazol como os compostos de maior ação inibitória frente à células vero infectadas e ao parasita intracelular, evidenciado uma futura aplicação desses derivados como agentes anti-T. gondii. Por fim, foram realizados testes antimicrobianos, os quais revelaram fracas atividades dos compostos sintetizados frente a fungos e bactérias. A descrição de atividades antimicrobianas na literatura, para compostos contendo os heterociclos imidazol, 1,3,4-tiadiazol e 4-tiazolidinona, justificou a realização dos testes para as moléculas obtidas
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Books on the topic "Imidazo [4"

1

Kawamoto, Yusuke. Synthesis and Biological Evaluation of Pyrrole–Imidazole Polyamide Probes for Visualization of Telomeres. Springer Singapore, 2019. http://dx.doi.org/10.1007/978-981-13-6912-4.

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Russia) Mezhdunarodnai︠a︡ molodezhnai︠a︡ nauchno-prakticheskai︠a︡ konferent︠s︡ii︠a︡ po svi︠a︡zi︠a︡m s obshchestvennostʹi︠u︡ (5th 2009 Kirov. Imidzh territoriĭ kak obshchestvennyĭ kapital: Materialy V Mezhdunarodnoĭ molodezhnoĭ nauchno-prakticheskoĭ konferent︠s︡ii po svi︠a︡zi︠a︡m s obshchestvennostʹi︠u︡, 3-4 dekabri︠a︡ 2009 g. Kirovskiĭ filial Peterburgskogo gumanitarnogo universiteta profsoi︠u︡zov, 2010.

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Book chapters on the topic "Imidazo [4"

1

Abe, Jiro. "Fast Photochromism of Bridged Imidazole Dimers." In New Frontiers in Photochromism. Springer Japan, 2013. http://dx.doi.org/10.1007/978-4-431-54291-9_9.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of dinuclear cobalt(II) chloride complex of 1, 2, 4, 5-tetrakis(4, 5-dihydro-imidazol-2-yl)-benzene." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-53971-2_289.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of dinuclear cobalt(II) bromide complex of 1, 2, 4, 5-tetrakis(4, 5-dihydro-imidazol-2-yl)-benzene." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-53971-2_290.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of dinuclear cobalt(II) chloride complex of 1, 2, 4, 5-tetrakis(4, 5-dihydro-imidazol-2-yl)-benzene." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-53971-2_291.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of dinuclear cobalt(II) bromide complex of 1, 2, 4, 5-tetrakis(4, 5-dihydro-imidazol-2-yl)-benzene." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-53971-2_292.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of mangenese(II) complex with [4-{2-((5-nitrosalicylidene)amino)ethyl}imidazole]." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-54228-6_430.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of polymeric manganese(II) complex with [4-{2-((5-nitrosalicylidene)amino)ethyl}imidazole]." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-54228-6_431.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of binuclear bis(acetylacetonato) chromium(III) complex bridged by imidazole-4, 5-dicarboxylate." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-49202-4_506.

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Pardasani, R. T., and P. Pardasani. "Magnetic properties of linear trinuclear manganese(II) complex with [4-{2-(5-nitrosalicylidene)amino)ethyl}imidazole]." In Magnetic Properties of Paramagnetic Compounds. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-54228-6_498.

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Aida, Toshimitsu, Hiroshi Abe, Kouichi Tokuda, and Shinji Sugimoto. "Potentiation of 3-(4-Amino-2-Methyl-5-Pyrimidinyl) Methyl-1-(2-Chloroethyl)-Nitrosourea Cytotoxicity in Resistant Human Glioma Cell by Pretreatment with 5-(3-Methyl-1-Triazeno) Imidazole-4-Carboxamide." In Biological Aspects of Brain Tumors. Springer Japan, 1991. http://dx.doi.org/10.1007/978-4-431-68150-2_31.

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Conference papers on the topic "Imidazo [4"

1

Bruna Schoenberger Teixeira and Lilian Tatiani Dusman Tonin. "Preparação de derivados 6-carbometóxi 4-(4-metóxifenil- e 4-hidroxifenil)imidazo[4,5-c]4,5,6,7-tetraidropiridina e 4-(4-metóxifenil-imidazo[4,5-c]piridina: otimização das condições reacionais." In XX Seminário de Iniciação Científica e Tecnológica da UTFPR. Universidade Tecnológica Federal do Paraná - UTFPR, 2015. http://dx.doi.org/10.20906/cps/sicite2015-0374.

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Nikhila, G. R., S. R. Batakurki, and B. C. Yallur. "Synthesis, characterization and antioxidant studies of benzo[4, 5]imidazo[2, 1-b]thiazole derivatives." In PROCEEDINGS OF INTERNATIONAL CONFERENCE ON ADVANCES IN MATERIALS RESEARCH (ICAMR - 2019). AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0023101.

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Jeniffer do Nascimento Ascencio Camargo and Lilian Tatiani Dusman Tonin. "Preparação de derivados 6-carbometóxi-4-fenil- e 4-N,N-dimetilaminofenil- imidazo[4,5-c]4,5,6,7-tetraidropiridina: otimização das condições reacionais." In XX Seminário de Iniciação Científica e Tecnológica da UTFPR. Universidade Tecnológica Federal do Paraná - UTFPR, 2015. http://dx.doi.org/10.20906/cps/sicite2015-0404.

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Wang, Linxiao, Wei Lu, Zhen Xiao, Min Zhou, Jiqing Li, and Shan Xu. "Synthesis of 1-(4-bromo-2-fluorophenyl)-1,3-dihydro-2H-imidazo[4,5-c] pyridin-2-one." In 2016 4th International Conference on Mechanical Materials and Manufacturing Engineering. Atlantis Press, 2016. http://dx.doi.org/10.2991/mmme-16.2016.91.

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Jin, Meizhong, Prafulla Gokhale, Andy Cooke, et al. "Abstract 3900: Discovery of FQIT: An imidazo[5,1-f][1,2,4]triazine derived dual IGF-1R/IR inhibitor." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-3900.

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Hosmane, Ramachandra, та Huan-Ming Chen. "Synthesis of 1-(2'-Deoxy-γ-D-ribofuranosyl)-1H-imidazo[4,5-d]pyridazine-4,7(5 H,6H)-dion: a Potentially Beneficial Building Block for Antisense Applications". У The 4th International Electronic Conference on Synthetic Organic Chemistry. MDPI, 2000. http://dx.doi.org/10.3390/ecsoc-4-01926.

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Hosmane, Ramachandra, та Huan-Ming Chen. "Synthesis of 1-(2'-O-Methyl-γ -D-Ribofuranosyl)-1H-imidazo[4,5-d]pyridazine-4,7(5H,6H)-dion: an Attractive Building Block for Antisense and Triple-helical Applications". У The 4th International Electronic Conference on Synthetic Organic Chemistry. MDPI, 2000. http://dx.doi.org/10.3390/ecsoc-4-01925.

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"Antimicrobial Activity of 2-Nitro-6-[(4-Phenyl-Benzo[4,5]imidazo[1,2-a] Pyrimidin-2-ylimino)-Methyl]-Phenol: A Novel Schiff Base Compound." In Nov. 27-28, 2017 South Africa. EARES, 2017. http://dx.doi.org/10.17758/eares.eap517211.

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Montaño, Rocío, and Murali Venkata Unnamatla. "Efficient and rapid conversion of 3-amino imidazo[1,2-a] pyridin-2-yl)-4H-chromene-4-ones to its corresponding thio analogues using Lawesson’s reagent ." In The 22nd International Electronic Conference on Synthetic Organic Chemistry. MDPI, 2018. http://dx.doi.org/10.3390/ecsoc-22-05668.

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Manabe, S., H. Yanagisawa, S. Ishikawa, et al. "TRYPTOPHAN PYROLYSIS PRODUCTS FOUND IN COOKED FOODS INHIBIT HUMAN PLATELET AGGREGATION BY INHIBITING CYCLOOXYGENASE." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643402.

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Humans are exposed to numerous toxic compounds in foods. During the past decade, several carcinogenic heterocyclic amines have been reported to be present in the cooked foods. Recently, we reported that some of the carcinogenic heterocyclic amines isolated from foods were present in human plasma. In order to know the effects of the carcinogens isolated from foods on the cell function, we investigated the effects of the carcinogenic heterocyclic amines including Trp-P-1(3-amino-l,4-dimethyl-5H-pyrido❘4,3-b❘indole) and Trp-P-2(3-amino-1-methyl-5H-pyrido❘4,3-b❘indole) on human platelet aggregation and polymorphonuclear leukocyte aggregation. Only tryptophan pyrolysis products, Trp-P-1 and Trp-P-2, had potent inhibitory effects on human platelet aggregation when platelets were preincubated with the carcinogens for 15 min. Other carcinogenic heterocyclic amines such as glutamic acid pyrolysates (Glu-P-1 and Glu-P-2) and 3H-imidazo ❘4,5-f❘quinoline-2-amines(IQ and MelQ) did show no effect on platelet aggregation even at 100 μM.The autoradiogram demonstrated that Tryptophan pyrolysis products, Trp-P-1 and Trp-P-2, dose-dependently inhibited the formation of HHT,PGD2,PGE2 and TXB2 induced by sodium arachidonate in human platelets labeled with ❘ 14c❘ arachidonic acid. Moreover, Trp-P-1 and Trp-P-2 did not show significant effects on leukocyte aggregation induced by sodium arachidonate (0.75mM) even at lOOnM. It is concluded that Trp-P-1 and Trp-P-2 isolated from cooked foodstuffs have potent inhibitory effects on the cyclo-oxygenase pathway of the platelet. Therefore, human platelet function might be affected with daily foods containing tryptophan pyrolysis products in vivo.
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