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Статті в журналах з теми "Triazole isosters"
Franco, Daiana Portella, Lucas Caruso, Nathalia Fonseca Nadur, Thiago Moreira Pereira, Renata Barbosa Lacerda, and Arthur Eugen Kümmerle. "Recent Advances in Microwave-Assisted Synthesis and Functionalization of 1,2,3- and 1,2,4-triazoles." Current Organic Chemistry 25, no. 23 (December 16, 2021): 2815–39. http://dx.doi.org/10.2174/1385272825666211011111408.
Повний текст джерелаSahu, Adarsh, Preeti Sahu, and Ramkishore Agrawal. "A Recent Review on Drug Modification Using 1,2,3-triazole." Current Chemical Biology 14, no. 2 (November 19, 2020): 71–87. http://dx.doi.org/10.2174/2212796814999200807214519.
Повний текст джерелаPanja, Atanu, and Kumaresh Ghosh. "Triazole-amide isosteric pyridine-based supramolecular gelators in metal ion and biothiol sensing with excellent performance in adsorption of heavy metal ions and picric acid from water." New Journal of Chemistry 43, no. 2 (2019): 934–45. http://dx.doi.org/10.1039/c8nj04380a.
Повний текст джерелаAlagodla, Ramesh, Paturu Rama Subba Reddy, Sravanthi Vemireddy, Devdutt Chaturvedi, and Halmuthur M. Sampath Kumar. "Synthesis of Novel 1,2,3-Triazolyl L-Serinol Palmitoyl Muramyl Dipeptide Derivatives." Asian Journal of Chemistry 35, no. 3 (2023): 763–70. http://dx.doi.org/10.14233/ajchem.2023.27553.
Повний текст джерелаWu, Jun, Nikolaos Kaplaneris, Shaofei Ni, Felix Kaltenhäuser, and Lutz Ackermann. "Late-stage C(sp2)–H and C(sp3)–H glycosylation of C-aryl/alkyl glycopeptides: mechanistic insights and fluorescence labeling." Chemical Science 11, no. 25 (2020): 6521–26. http://dx.doi.org/10.1039/d0sc01260b.
Повний текст джерелаRečnik, Lisa-Maria, Wolfgang Kandioller, and Thomas L. Mindt. "1,4-Disubstituted 1,2,3-Triazoles as Amide Bond Surrogates for the Stabilisation of Linear Peptides with Biological Activity." Molecules 25, no. 16 (August 6, 2020): 3576. http://dx.doi.org/10.3390/molecules25163576.
Повний текст джерелаWales, Steven M., Katherine A. Hammer, Amy M. King, Andrew J. Tague, Dena Lyras, Thomas V. Riley, Paul A. Keller, and Stephen G. Pyne. "Binaphthyl-1,2,3-triazole peptidomimetics with activity against Clostridium difficile and other pathogenic bacteria." Organic & Biomolecular Chemistry 13, no. 20 (2015): 5743–56. http://dx.doi.org/10.1039/c5ob00576k.
Повний текст джерелаTautz, Markus, Juan Torras, Santiago Grijalvo, Ramón Eritja, César Saldías, Carlos Alemán, and David Díaz Díaz. "Expanding the limits of amide–triazole isosteric substitution in bisamide-based physical gels." RSC Advances 9, no. 36 (2019): 20841–51. http://dx.doi.org/10.1039/c9ra03316e.
Повний текст джерелаTautz, Markus, César Saldías, Antonio Diego Lozano-Gorrín, and David Díaz Díaz. "Use of a bis-1,2,3-triazole gelator for the preparation of supramolecular metallogels and stabilization of gold nanoparticles." New Journal of Chemistry 43, no. 35 (2019): 13850–56. http://dx.doi.org/10.1039/c9nj03427g.
Повний текст джерелаJunaid, Lim, Zhou, Chui, and Dolzhenko. "Fused Heterocyclic Systems with an s-Triazine Ring. 34. Development of a Practical Approach for the Synthesis of 5-Aza-isoguanines." Molecules 24, no. 8 (April 12, 2019): 1453. http://dx.doi.org/10.3390/molecules24081453.
Повний текст джерелаДисертації з теми "Triazole isosters"
Ostric, Adrian. "Hydroxyethylene isosters of Xaa-Pro dipeptides: synthetic approaches and new HIV-PR inhibitors." Doctoral thesis, Università degli studi di Trieste, 2011. http://hdl.handle.net/10077/4576.
Повний текст джерелаThe aspartic protease (HIV-Pr) of the human immunodeficiency virus, responsible agent for AIDS, is surely one of the most studied enzymes in terms of structure and activity. HIV-Pr is responsible for cleaving the viral polyprotein precursor into structural proteins and enzymes and plays an essential role in the viral replication and maturation. HIV-Pr has thus become the target of numerous efforts to design antiviral therapeutic agents suitable for the treatment of AIDS. In the field of organic chemistry, the search for effective HIV-Pr inhibitors has boosted the development of new methodologies for the stereoselective synthesis of compounds containing multiple chiral centers, on which reversible inhibitors are generally based. HIV-Pr shows peculiar characteristics as it is able, unlike any other eukaryotic aspartic protease, to hydrolyze amide bonds with proline as the N-terminal residue. Moreover, it is active in a dimeric form, possessing C2 symmetry, in which each monomer contributes a catalytic aspartate. The first part of the present doctoral work described in Chapter 2, has been dedicated to the synthesis of hydroxyethylene Phe-Pro isosters in which the pyrrolidine ring is expanded by a condensed aromatic ring in order to provide a better fit to the enzyme’s catalytic site. During the synthesis of the isoster a novel reaction was discovered in which enaminones are directly formed by treatment of α,β-unsaturated ketones with trimethylsilylazide and fluoride. Phe-Pro isosters based on the enaminone structure showed moderate activity as HIV-Pr inhibitors. The direct amination of α,β-unsaturated ketones is the subject of Chapter 3. This reaction is demonstrated to be general for enones containing a β-hydrogen. A mechanism based on azide activation via formation of a pentacoordinated silicon species followed by a 1,3-dipolar cycloaddition is proposed and supported by experimental results and calculations. In Chapter 4 is reported the synthesis of a library of triazole inhibitors by a combinatorial approach based on click chemistry. The library was screened for HIV-Pr inhibition and deconvoluted. A set of promising members from the library was synthesized as single, enantiomerically pure compounds that confirmed to be active HIV-Pr inhibitors. Finally, in Chapter 5 the development of an alternative approach to dipeptide isosters, based on the ring closing metathesis of aminoacid-derived allylamines, is described. Building of the four carbon atom backbone of the isosteres is obtained after mounting the olefins on designed linkers that allow selectivity in the cross metathesis, and easy final cleavage. Carbamate linkers will also allow also protection of the amino groups during the next steps of the synthesis leading to the desired di- and monohydroxyethylene isosters.
La proteasi aspartica (HIV-PR) del virus della immunodeficienza umana, l'agente responsabile dell'AIDS, è sicuramente uno degli enzimi più studiati in termini di struttura e di attività. HIV-Pr è responsabile della scissione della poliproteina virale in proteine strutturali ed enzimi e svolge un ruolo essenziale nella replicazione e maturazione del virus. HIV-Pr è così diventato il bersaglio di numerosi studi mirati alla progettazione di agenti terapeutici antivirali adatti per il trattamento dell'AIDS. Nel campo della chimica organica, la ricerca di efficaci inibitori dell'HIV-Pr ha stimolato lo sviluppo di nuove metodologie per la sintesi stereoselettiva di composti contenenti più centri chirali, che costituiscono la base strutturale della maggior parte degli inibitori reversibili. HIV-Pr presenta caratteristiche peculiari in quanto è in grado, unica tra le proteasi aspartiche da eucarioti, di idrolizzare legami ammidici con la prolina come residuo N-terminale. Inoltre, l’enzima è attivo in una forma dimerica, con simmetria C2, in cui ogni monomero contribuisce con un residuo catalitico di acido aspartico. La prima parte del presente lavoro di dottorato, descritta nel capitolo 2, è stata dedicata alla sintesi di isosteri idrossietilenici del dipeptide Phe-Pro, contenenti un anello pirrolidinico espanso al fine di migliorare le interazioni con il sito catalitico dell'enzima. Durante la sintesi dell’ isostere è stata scoperta una nuova reazione di formazione di enaminoni per trattamento di chetoni α,β-insaturi con trimethylsilylazide e fluoruro. Alcuni isosteri Phe-Pro basati sulla struttura enaminonica hanno mostrato una moderata attività come inibitori della HIV-PR. L'amminazione diretta di chetoni -insaturi è il soggetto del capitolo 3. Questa reazione si è dimostrata essere generale per enoni contenente un idrogeno in posizione β. Un meccanismo basato sulla attivazione della azide attraverso la formazione di una specie pentacoordinata di silicio seguita da una cicloaddizione 1,3-dipolare viene proposto sulla base dei risultati sperimentali e di calcoli teorici. Nel capitolo 4 è riportata la sintesi di una libreria di inibitori triazolici ottenuti con un approccio combinatoriale. La libreria è stato analizzata per l'inibizione di HIV-Pr e deconvoluta. Alcuni membri promettenti della biblioteca sono stati sintetizzati come composti singoli, in forma enantiomericamente pura, confermandosi attivi inibitori della HIV-PR. Infine, nel capitolo 5, é descritto lo sviluppo di un approccio alternativo a isosteri di dipeptidi, basato sulla “ring closing methatesis” di allilamine derivate da aminoacidi. La costruzione dello scheletro degli isosteres si ottiene dopo l’assemblaggio delle olefine su un nuovo linker che consente una cross-metatesi selettività nonché un facile distacco del prodotto. Il linker può anche essere utilizzato come gruppo proteggente nella successiva elaborazione sintetica dei prodotti.
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Stockdale, David Paul. "The synthesis of isosteres of pawhuskin- and schweinfurthin-based stilbenes." Diss., University of Iowa, 2017. https://ir.uiowa.edu/etd/5999.
Повний текст джерелаChemama, Maryline. "Synthèse d'analogues d'aminoacyl-ARNt pour l'étude et l'inhibition d'une transférase de type Fem." Paris 6, 2009. http://www.theses.fr/2009PA066731.
Повний текст джерелаMonceaux, Christopher Jon. "Triazole-linked reduced amide isosteres: An approach for the fragment-based drug discovery of anti-Alzheimer's BACE1 inhibitors and NH-assisted Fürst-Plattner opening of cyclohexene oxides." Diss., Virginia Tech, 2010. http://hdl.handle.net/10919/30221.
Повний текст джерелаPh. D.