Relevant bibliographies by topics / Pyrazole derivates

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Academic literature on the topic 'Pyrazole derivates'

Author: Grafiati
Published: 4 June 2021
Last updated: 8 February 2022

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Journal articles on the topic "Pyrazole derivates"

1

Ardiansah, Bayu. "A RECENT UPDATE: ANTIMICROBIAL AGENTS CONTAINING PYRAZOLE NUCLEUS." Asian Journal of Pharmaceutical and Clinical Research 11, no. 12 (December 7, 2018): 88. http://dx.doi.org/10.22159/ajpcr.2018.v11i12.29418.

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Objective: In this review, we report antimicrobial candidates containing pyrazole nucleus integrated with various functionalities.Methods: research results by numerous scientists have been summarized from international journals indexed in reputed database such as Scopus and Web of Science.Results: Pyrazole derivatives are much of interest as potent bioactive molecules. They have shown large bioactivities especially antimicrobial performance against broad spectrum of bacterial strains.Conclusion: Several designed pyrazole derivates possessed good to superior antimicrobial activities.
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2

Abaszadeh, Mehdi, Hassan Sheibani, and Kazem Saidi. "The Condensation of (Chlorocarbonyl)phenyl Ketene with Bisnucleophiles. Synthesis of 4-Hydroxy-5-phenylpyro-[2,3-c]pyrazol-6-ones and Formation of Pyrazolo[1,2-a]pyrazole-triones by Hydrogen Exchange in Unstable Mesoionic Compounds." Australian Journal of Chemistry 63, no. 1 (2010): 92. http://dx.doi.org/10.1071/ch09344.

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The addition of (chlorocarbonyl)phenyl ketene 2 to 5-alkylpyrazol-3(4H)-ones 1 led to the formation of 3-hydroxypyrazolo[1,2-a]pyrazole-dione/pyrazolo[1,2-a]pyrazole-trione derivatives 3. This is ascribed to hydrogen exchange in initially formed unstable, mesoionic pyrazolo[1,2-a]pyrazol-4-ium-5-olates. In contrast, condensation of the same ketene with 3-alkyl-1-phenyl-2-pyrazolin-5-ones 4 afforded 4-hydroxy-3-alkyl-1,5-diphenylpyrano[2,3-c]pyrazol-6-one derivatives 5. The latter reaction provides a new and rapid route to 4-hydroxy-2-pyrones fused to pyrazole rings, in good to excellent yields.
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3

Lerner, Hans-Wolfram, Günter Margraf, Tonia Kretz, Olav Schiemann, Jan W. Bats, Gerd Dürner, Fabrizia Fabrizi de Biani, Piero Zanello, Michael Boltea, and Matthias Wagner. "Redox Behaviour of Pyrazolyl-Substituted 1,4-Dihydroxyarenes: Formation of the Corresponding Semiquinones, Quinhydrones and Quinones." Zeitschrift für Naturforschung B 61, no. 3 (March 1, 2006): 252–64. http://dx.doi.org/10.1515/znb-2006-0304.

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Abstract Pyrazolyl-substituted 1,4-dihydroxybenzene and 1,4-dihydroxynaphthene derivatives have been synthesized by reaction of 1,4-benzoquinone and 1,4-naphthoquinone, respectively, with pyrazole. Cyclovoltammetric measurements have shown that 1,4-benzoquinone possesses the potential to oxidize 2-(pyrazol-1-yl)- and 2,5-bis(pyrazol-1-yl)-1,4-dihydroxybenzene. The 2,5-bis(pyrazol-1-yl)- 1,4-dihydroxybenzene reacts with air to give quantitatively black insoluble 2,5-bis(pyrazol-1-yl)-1,4- quinhydrone. Black crystals of 2,5-bis(pyrazol-1-yl)-1,4-quinhydrone suitable for X-ray diffraction were grown from methanol at ambient temperature (monoclinic C2/c). The poor yields of pyrazolylsubstituted 1,4-dihydroxybenzene and 1,4-dihydroxynaphthene derivatives can be explained by the formation of insoluble black quinhydrons in the reaction of benzoquinone and naphthoquinone with pyrazole. The dianions of 2-(pyrazol-1-yl)- and 2,5-bis(pyrazol-1-yl)-1,4-dihydroxybenzene react with oxygen to give the corresponding semiquinone anions. 2,5-Bis(pyrazol-1-yl)-1,4-benzoquinone shows two reversible one-electron reduction processes in cyclovoltammetric measurements, whereas pyrazolyl-substituted 1,4-dihdroxybenzene and -naphthene derivatives undergo irreversibile electrontransfer processes.
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Alsayari, Abdulrhman, Abdullatif Bin Muhsinah, Yahya I. Asiri, Jaber Abdullah Alshehri, Yahia N. Mabkhot, Mohammad Y. Alfaifi, Serag Eldin I. Elbehairi, Mater H. Mahnashi, and Mohd Zaheen Hassan. "Arylhydrazono/Aryldiazenyl Pyrazoles: Green One-Pot Solvent-Free Synthesis and Anticancer Evaluation." Letters in Organic Chemistry 17, no. 10 (November 17, 2020): 772–78. http://dx.doi.org/10.2174/1570178617666200320104923.

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The aim of this study was to synthesize and evaluate the biological activity of pyrazole derivatives, in particular, to perform a “greener” one-pot synthesis using a solvent-free method as an alternative strategy for synthesizing hydrazono/diazenyl-pyridine-pyrazole hybrid molecules with potential anticancer activity. Effective treatment for all types of cancers is still a long way in the future due to the severe adverse drug reactions and drug resistance associated with current drugs. Therefore, there is a pressing need to develop safer and more effective anticancer agents. In this context, some hybrid analogues containing the bioactive pharmacophores viz. pyrazole, pyridine, and diazo scaffolds were synthesized by one-pot method. Herein, we describe the expedient synthesis of pyrazoles by a onepot three-component condensation of ethyl acetoacetate/acetylacetone, isoniazid, and arenediazonium salts under solvent-free conditions, and the evaluation of their cytotoxicity using a sulforhodamine B assay on three cancer cell lines. Molecular docking studies employing tyrosine kinase were also carried out to evaluate the binding mode of the pyrazole derivatives under study. 1-(4-Pyridinylcarbonyl)-3- methyl-4-(2-arylhydrazono)-2-pyrazolin-5-ones and [4-(2-aryldiazenyl)-3,5-dimethyl-1H-pyrazol-1- yl]-4-pyridinylmethanones, previously described, were prepared using an improved procedure. Among these ten products, 1-isonicotinoyl-3-methyl-4-[2-(4-nitrophenyl)hydrazono]-2-pyrazolin-5-one (1f) displayed promising anticancer activity against the MCF-7, HepG2 and HCT-116 cell lines, with an IC50 value in the range of 0.2-3.4 μM. In summary, our findings suggest that pyrazoles containing hydrazono/ diazenyl and pyridine pharmacophores constitute promising scaffolds for the development of new anticancer agents.
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Mocanu, Anca Mihaela, Constantin Luca, and Alina Costina Luca. "Synthesis, Characterization and Thermal Degradation of Some New 3,5-dimethyl Pyrazole Derivatives." Revista de Chimie 68, no. 2 (March 15, 2017): 317–22. http://dx.doi.org/10.37358/rc.17.2.5444.

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The purpose of this research is to synthetize, characterize and thermal degradation of new heterolytic derivates with potential biological properties. The derivates synthesis was done by obtaining new molecules with pyralozone structure which combine two pharmacophore entities: the amidosulfonyl-R1,R2 phenoxyacetil with the 3,5-dimethyl pyrazole which can have potential biological properties. The synthesis stages of the new products are presented as well as the elemental analysis data and IR, 1H-NMR spectral measurements made for elucidating the chemical structures and thermostability study which makes evident the temperature range proper for their use and storage. The obtained results were indicative of a good correlation of the structure with the thermal stability as estimated by means of the initial degradation temperatures as well as with the degradation mechanism by means of the TG-FTIR analysis.
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Sophy, Mohamed Ahmed Elian, and Mohamed Ahmed Mahmoud Abdel Reheim. "Synthesis of Some New 1, 3, 4-Oxadiazole, Pyrazole, and Pyrimidine Bearing Thienopyrazole Moieties." Current Organic Synthesis 17, no. 8 (October 28, 2020): 661–70. http://dx.doi.org/10.2174/1570179417999200730215318.

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Aim and Objective: According to the literature survey, pyrazole is a unique template that is associated with several biological activities. This article highlighted the research work of many researchers reported in the literature for synthesis and different pharmacological activities of the pyrazole nucleus. In the present work, pyrazol- 3-one 1 was reacted with cyanoacetic acid hydrazide and elemental sulfur to afford the corresponding thieno[3,2-c]pyrazol-6-carbohydrazide 3 derivatives. The latter compound reacted with some electrophilic reagents such as DMF-DMA, triethylorthoformate, arylidenemalononitriles and chalcones under neat conditions to give substituted oxadiazole and pyrazole, respectively. The treatment of compound 3 with active methylene reagents such as acetylacetone, diethylmalonate, ethyl acetoacetate and ethyl cyanoacetate under suitable conditions afforded pyrazole derivatives 10, 11, 13, and 15, respectively. Novel pyrazolothienopyrimidine 27 and 30 were prepared from precursor 26 with carbon disulfide and triethylorthoformate, respectively. The chemical structures of the newly synthesized compounds were established by elemental and spectral analyses including IR, and 1HNMR in addition to 13C-NMR and mass spectra. Materials and Methods: A novel substituted pyrazole, pyrimidine and pyrazolothienopyrimidine were obtained via Gewald synthesis of thiophene and fused thiophene and Mannich reactions of 5-amino-3-phenyl-1Hthieno[ 3,2-c]pyrazole-6-carbohydrazide. Results and Discussion: A series of some newly azoles and azines were prepared via reaction of thieno[3,2- c]pyrazol-6-carbohydrazide derivative 3 as starting material with some electrophilic and nucleophilic reagents. The structures of target compounds were established by elemental analyses and spectral data. Conclusion: Pyrazole is a unique template that is associated with several biological activities. This article highlighted the research work of many researchers reported in the literature for synthesis and different pharmacological activities of the pyrazole nucleus. In the current investigation, we have developed new and efficient methods for the synthesis of thieno[3,2-c]pyrazol-6-carbohydrazide derivatives. In addition, we have explored the preparative potential of these substances as intermediates for the synthesis of substituted pyrazoles and fused pyrazoles 10-30, respectively.
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Alsayari, Abdulrhman, Yahya I. Asiri, Abdullatif Bin Muhsinah, and Mohd Zaheen Hassan. "Anticolon Cancer Properties of Pyrazole Derivatives Acting through Xanthine Oxidase Inhibition." Journal of Oncology 2021 (July 5, 2021): 1–5. http://dx.doi.org/10.1155/2021/5691982.

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Background. Pyrazoles are an interesting class of compounds showing potent anticancer activities. Our previous studies have demonstrated the potent anticancer activity of pyrazole analogues. Therefore, we focused on developing anticancer agents through structure optimization of the pyrazolyl lead molecule. Methods. The pyrazole derivatives were prepared by the appropriate synthetic protocols. The antiproliferative activities were evaluated using a sulforhodamine B assay against three cancer cell lines. In vitro and in silico molecular docking studies employing xanthine oxidase were used to explore the mechanism by which pyrazole derivatives exert anticancer effects. Results. One of the pyrazole derivatives demonstrated the greatest promise as an anticancer agent against the human colon cancer cell line (IC50 4.2 μM), with a potent xanthine oxidase inhibitory activity (IC50 0.83 μM). Conclusion. In summary, our findings suggest that these pyrazolyl analogues containing a pyridine nucleus could serve as a promising lead molecule in the development of novel anticancer agents.
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Farooq, Saba, and Zainab Ngaini. "Chalcone Derived Pyrazole Synthesis via One-pot and Two-pot Strategies." Current Organic Chemistry 24, no. 13 (October 1, 2020): 1491–506. http://dx.doi.org/10.2174/1385272824999200714101420.

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Pyrazole is an imperative heterocyclic molecule in the synthetic and medicinal fields. Pyrazole is stable compound that is particularly used in pharmaceutical applications (i.e., anticancer, antifungal, antiviral, antimicrobial and antioxidant) and electronic industries. This review depicted the synthesis of pyrazoles derivatives by employing chalcone derivatives as a starting material via one and two-pot strategies. The one-pot strategy is an exclusive method for chalcone cyclization and oxidation, while two-pot strategy is reported through the preparation of chalcone derivatives, i.e., pyrazoline, hydrazone and bromochalcone prior to the synthesis of pyrazole. One-pot strategy is frequently reported for pyrazole synthesis purposes due to unique, stable, reactive and well-known chalcone reactants having easy handing then two-pot strategy. This review is momentous in organic chemistry, especially synthesis related to pyrazole and drug industry.
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Hrynyshyn, Yevhenii, Hanna Musiichuk, Olena Komarovska-Porokhnyavets, Oksana Is’kiv, Nataliia Moskalenko, Maryna Stasevych, Nazar Tsyzoryk, and Mykhailo Vovk. "Synthesis and Antimicrobial Activity of 4-Arylthio- and 4 Alkylthiofunctionalized Pyrazolo[1,5-a]pyrazines." Ukrainian Chemistry Journal 85, no. 1 (February 15, 2019): 58–66. http://dx.doi.org/10.33609/0041-6045.85.1.2019.58-66.

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The reaction of pyrazolo[1,5-a]pyrazine-4(5H)ones with phosphorus tribromoxide in boiling benzene yielded 4-bromopyrazolo[1,5-a]pyrazines, and the thionation with phosphorus pentasulfide in pyridine at 90 °C led to pyrazolo[1,5-a]pyrazine-4(5H)thiones. The synthesized bromine derivatives are electrophilic, and thiones are nucleophilic substrates. Their subsequent structural modification in the first case was carried out by interaction with thiophenols, and in the second case was conducted with functional halogenoalkanes. It was shown that bromides react with substituted thiophenols in dimethylformamide in the presence of potassium carbonate at 90 °C to form 4-arylthiopyrazolo[1,5-a]pyrazines with yields of 65–83 %. 4-S-methyl-functionalized derivatives of pyrazole[1,5-a]pyrazines with yields of 60–78 % were easily obtained by the alkylation of pyrazole[1,5-a]pyrazin-4(5H)thiones with a-bromoketones, bromoacetic acid, ethyl bromoacetate and bromoacetonitrile in the K2CO3—DMF system at room temperature. The composition of all synthesized compounds is in agreement with the results of elemental analysis and mass spectra. Their structure is confirmed by NMR 1H and 13C spectra. In particular, in the NMR 1H spectra of 4-arylthiopyrazolo[1,5-a]pyrazines, in addition to the characteristic signals of the pyrazole and pyrazine nuclei, signals of protons of thioaryl substituents are present in the range of 7.04 –8.05 ppm, and in NMR spectra of the 1H 4-S-methylfunctionalized derivatives of pyrazole[1,5-a]pyrazines signals of exocyclic methylene protons are present at 4.11– 5.02 ppm. Promising derivatives with antibacterial activity against the test cultures S. aureus (MIC = 7.8 g/mL), M. luteum (MIC = 3.9 g/mL), and antifungal activity against the test culture of fungus A. niger (MIC = 7.8 g/mL) were determined among 4-S-substituted pyrazole[1,5-a]pyrazines as a result of studies of the antimicrobial activity.
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Edrees, Mastoura M. "Synthesis of 4-hydrazinopyrazolo[3,4-d]pyrimidines and their Reactions with Carbonyl Compounds." Journal of Chemical Research 37, no. 1 (January 2013): 6–10. http://dx.doi.org/10.3184/174751912x13543818811749.

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Synthesis of a new 4-hydrazinopyrazolo[3,4- d]pyrimidine was achieved via heating (4,6-dithioxo-1 H-pyrazolo[3,4- d] pyrimidin-3-yl)acetonitrile with hydrazine hydrate. Reactions of the latter product with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues afforded the corresponding hydrazone and pyrazole derivatives, respectively. Similarly, condensation of 2-[6-(benzylsulfanyl)-4-hydrazino-1 H-pyrazolo[3,4- d]pyrimidin-3-yl]acetonitrile with thiophene-2-carbaldehyde and ethyl hydrazonoacetoacetate analogues gave the respective hydrazone and pyrazolone derivatives. Alkylation reactions of 2-[4,6-bis(benzylsulfanyl)-1 H-pyrazolo[3,4- d]pyrimidin-3-yl]acetonitrile with arylamines gave the respective 4-( N-arylamino)-6-benzylsulfanylpyrazolo[3,4- d]pyrimidine derivatives.
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Dissertations / Theses on the topic "Pyrazole derivates"

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Zouikri, Mohamed. "Le résidu aza-prolyle, son introduction dans un peptide : modifications structurales dues à la substitution AzPRO/PRO." Vandoeuvre-les-Nancy, INPL, 1996. http://www.theses.fr/1996INPL079N.

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Les azapeptides constituent une famille de pseudopeptides dans laquelle le groupe CHalpha d'un ou plusieurs résidus a été substitué par un atome d'azote isoélectronique. Bien que de nombreux analogues de peptides bioactifs aient été synthétisés et biologiquement testés, peu de travaux concernant leur structure spatiale ont été rapportés jusqu'a ce jour. Un des avantages de cette substitution est de garder intacte la nature chimique de la chaine latérale dont le rôle est si important, comme par exemple, dans les processus de reconnaissance moléculaire. De plus, nous avons choisi d'étudier l'analogue azaproline de la proline qui fait partie des acides aminés protéinogènes et qui, en tant qu'iminoacide, présente une forte singularité au sein de ces derniers. Pour introduire le résidu azaprolyle dans un peptide, nous avons mis au point un protocole de synthèse faisant appel au triphosgène. Contrairement aux méthodes utilisées et décrites dans la littérature, et qui préconisent l'emploi d'uréthanes activés nécessitant des conditions sévères (reflux pendant plusieurs heures), ce réactif permet de travailler à faible température et avec des temps de réaction raccourcis, en effectuant la chlorocarbonylation, soit de l'hydrazine précurseur (cycle pyrazolidine), soit de l'extrémité N-terminale du peptide en cours d'élongation par synthèse récurrente. Du point de vue conformationnel, AzPro se comporte à l'opposé de Pro. En effet, il induit un repliement (beta cis) avec le résidu qui le précède et non pas avec celui qui le suit. D’autre part, les atomes d'azote du cycle pyrazolidine, bien qu'acylés, sont partiellement sp3 et acquièrent ainsi une prochiralité. C’est le résidu qui précède AzPro qui impose sa propre chiralité à Nalpha du résidu AzPro et non pas la chaine C-terminale. Enfin, l'abolition de la contrainte de cycle dans le résidu N-méthyl-aza-alanyle, n'entraine pas un profond changement structural, mais l'apparition minoritaire de conformères plus flexibles
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2

Nakhai, Azadeh. "Synthetic studies of nitrogen containing heterocycles, particularly pyrazole and benzotriazine derivatives." Stockholm, 2009. http://diss.kib.ki.se/2009/978-91-7409-687-3/.

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3

Gormen, Meral. "Synthesis Of Ferrocenyl Substituted Pyrazoles." Master's thesis, METU, 2005. http://etd.lib.metu.edu.tr/upload/3/12606358/index.pdf.

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Pyrazoles have been studied for over a century as an important class of heterocyclic compounds and continue to attract considerable interest due to the broad range of biological activities they possess. The incorporation of the essential structural features of pyrazoles with a ferrocene moiety could provide new derivatives with unexpected and/or enhanced biological activities since several ferrocene derivatives have already been shown to be active against a number of tumors. For this reason, we investigated the synthesis of ferrocenyl-substituted pyrazoles, such as 1-alkyl/aryl-5-ferrocenylpyrazoles, by employing the reaction between (2-formyl-1-chlorovinyl)ferrocene and hydrazine derivatives. Although this reaction is known, it was not studied in much detail and the low yields of ferrocenyl pyrazoles were obtained. Thus, we have reinvestigated this reaction and improved the yields of pyrazoles by optimizing the reaction conditions. (2-Formyl-1-chloro vinyl)ferrocene was first reacted with the excess amount (3 equivalents) of hydrazine derivative at 25 0C in dioxane under argon for 2 hours, and the resulting mixture was then heated at 100 0C for 6 hours in the same solvent. Under our optimized conditions, these reactions afforded 1-alkyl/aryl-5-ferrocenylpyrazole derivatives in moderate to good yields as a single or major product of the reaction. In some cases, 1-alkyl/aryl-3-ferrocenylpyrazole derivatives resulted from these reactions as very minor products.
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Dias, Sandra Isabel Godinho. "Synthesis and supramolecular phenomenon of novel pyrazine derivatives." Thesis, University of Kent, 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.429799.

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Yazici, Ceyda. "Synthesis Of 4-iodopyrazole Derivatives." Master's thesis, METU, 2008. http://etd.lib.metu.edu.tr/upload/3/12609750/index.pdf.

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Pyrazoles have been studied for over a century as an important class of heterocyclic compounds and continue to attract considerable interest due to the broad range of biological activities they possess. The electrophilic cyclization of the acetylenic hydrazones initiated by molecular iodine could provide new ways of synthesizing biologically active 4-iodopyrazole derivatives, which are important precursors for the synthesis of highly substituted pyrazole derivatives. For this reason, we investigated the synthesis of 4-iodopyrazole derivatives, such as 1-aryl- 5-alkyl/aryl-4-iodopyrazoles, starting from phenylhydrazine and ,-acetylenic aldehyde derivatives. Initially, ,-acetylenic aldehydes were synthesized by formylation reaction of corresponding alkynes with DMF. Then, hydrazone derivatives of these aldehydes were prepared by heating them with phenylhydrazine in a neat manner at 55 °
C for 5 h. Finally, acetylenic phenyl hydrazone derivatives were subjected to electrophilic cyclization by treating with excess molecular iodine at 80 °
C for 3 h. Although electrophilic cyclization is commonly used in organic chemistry, it has not been employed for the cyclization of acetylenic phenyl hydrazones to pyrazole derivatives. Under optimized conditions, these reactions afforded 1-aryl-5-alkyl/aryl-4-iodopyrazole derivatives in moderate to good yields as the single or the major product of the reactions. In some cases, 1-aryl-5-alkyl/arylpyrazole derivatives resulted from these reactions as minor products. In conclusion, 4-iodopyrazole derivatives were synthesized for the first time directly from acyclic starting materials, ,-acetylenic phenylhydrazones and iodine, via electrophilic cyclization.
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Vetica, Fabrizio [Verfasser]. "Organocatalytic Asymmetric Synthesis of Isochromanones, Tetranortriterpenoids and Pyrazolone Derivatives / Fabrizio Vetica." München : Verlag Dr. Hut, 2018. http://d-nb.info/1155056213/34.

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Despotopoulou, Christina. "Br/Mg-Exchange on 1,2-Dibromocyclopentene Derivatives and Regio- and Chemoselective Functionalizations of Pyrazoles and Related Heterocycles." Diss., lmu, 2009. http://nbn-resolving.de/urn:nbn:de:bvb:19-104233.

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Pasin, Juliana Saibt Martins. "Atividade antipirética e antiinflamatória de derivados 5-trifluormetil-4,5-diidro-1H-1-carboxiamida pirazol em ratos." reponame:Biblioteca Digital de Teses e Dissertações da UFRGS, 2010. http://hdl.handle.net/10183/28004.

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A febre é um aumento regulado da temperatura corporal central, caracterizada por uma alteração no centro termorregulatório, a qual resulta da interação entre o sistema nervoso central e o imunológico. Enquanto a febre caracteriza lesão celular, infecção e inflamação, ela tem sido considerada o mais importante componente da resposta de fase aguda. Embora existam evidências de que a febre aumenta a defesa do hospedeiro, alguns estudos têm sugerido que o aumento da temperatura central a níveis febris pode ser prejudicial. Portanto, nas situações clínicas nas quais os riscos associados com a febre superam os benefícios, o tratamento antipirético é formalmente indicado. Os derivados pirazolínicos constituem um importante grupo de compostos orgânicos que têm sido extensivamente estudados devido às suas inúmeras atividades biológicas, que incluem atividade antipirética. Recentemente uma série de derivados pirazolínicos inéditos foi avaliada quanto à atividade antiedematogênica e antinociceptiva em camundongos. Estes compostos causam antinocicepção no teste da formalina e no modelo de artrite induzida por adjuvante de Freund, bem como diminuem o edema induzido por carragenina. Dados os efeitos antiinflamatórios descritos para estes compostos, o objetivo do estudo foi investigar o efeito de oito derivados 5-trifluormetil-4,5-diidro- 1H-1-pirazol-1-carboxiamida (TFDPs) sobre a temperatura corporal basal, a febre induzida por S. cerevisiae (0.135 g/Kg, i.p.) e a inflamação peritoneal em ratos Wistar machos de 28 dias de idade. Somente os compostos 3Et- e 3Pr-TFDP (140 e 200 μmol/kg respectivamente, s.c., 4 h após a injeção do S. cerevisiae) atenuaram a febre em 61.0% e 82.4%, respectivamente. Estes dois compostos foram selecionados para a investigação dos mecanismos de ação. Os efeitos sobre a atividade da ciclooxigenase-1 e -2 (COX-1 e COX-2), a oxidação in vitro do 1,1-difenil-2- picrilhidrazil (DPPH), os níveis de TNF-a e IL-1b e influxo de leucócitos na cavidade peritoneal dos ratos injetados com S. cerevisiae foram determinados. Enquanto 3Et- e 3Pr-TFDP não alteraram o aumento nos níveis de TNF-a e IL-1b induzido por S. cerevisiae, o derivado 3Et- TFDP causou uma redução de 42% na contagem de leucócitos na cavidade peritoneal. 3Et- e 3Pr-TFDP não alteraram a atividade da COX-1 e COX-2 in vitro, mas apresentaram atividade antioxidante no ensaio do DPPH, com CI50 de 39.3 (25.0-62.0) mM e 162.9 (135.6-195.7) mM, respectivamente. Em outro grupo de experimentos, foi avaliado o efeito do pré-tratamento dos animais com os compostos 3Et- e 3Pr-TFDP sobre a inflamação peritoneal induzida por S.cerevisiae em ratos. O pré-tratamento com 3Et-TFDP (140 μmol/kg, 5 mL/Kg, s.c.) preveniu significativamente o aumento no influxo de leucócitos, a permeabilidade vascular peritoneal e a atividade da mieloperoxidase (MPO), mas não teve efeito sobre os níveis de TNF-a e IL-1b. Por outro lado, 3Pr-TFDP (200 μmol/kg, 5 mL/Kg, s.c.) não apresentou efeito sobre nenhum desses parâmetros inflamatórios. O presente estudo descreve dois novos derivados pirazolínicos com atividade antipirética, cujos mecanismos de ação não envolvem inibição da COX ou inibição da liberação de citocinas pirogênicas. Além disso, foi demonstrado que o composto 3Et-TFDP apresenta potencial antiinflamatório, atuando sobre o influxo de leucócitos, permeabilidade vascular peritoneal e aumento da atividade da MPO induzidos por S. cerevisiae. Em conjunto, nossos dados sugerem que os derivados pirazolínicos 3Et- e 3Pr-TFDP parecem ser compostos antipiréticos e antiinflamatórios promissores.
Fever is a regulated increase of body core temperature characterized by a raised thermoregulatory set point, which results from the interaction of the central nervous and immune systems. While fever is a hallmark of injury, infection and inflammation, it has also been considered the most important component of acute-phase response. Although there is evidence supporting the idea that fever enhances host defenses, some studies have suggested that raising core temperature to the febrile range may be harmful. Therefore, in the clinical situations in which fever-associated risks outweigh benefits, antipyretic treatment is formally indicated. Pyrazoles constitute an important group of organic compounds that have been extensively studied due to their numerous biological activities. Recently a series of pyrazole derivatives have been screened for antinociceptive and antiedematogenic activity in mice. These compounds cause antinociception in the formalin test and in the Freund's adjuvant (CFA) animal model of arthritis and decrease carrageenin-induced edema. Given the effects reported for these compounds, we decided to investigate the effect of eight 5-hydroxy-5-trifluoromethyl-4,5-dihydro- 1H-1-carboxyamidepyrazoles (TFDPs) on body temperature, baker´s yeast-induced fever and peritoneal inflammation in 28 days-old male Wistar rats. Only 3ethyl- and 3propyl-TFDP (140 and 200 μmol/kg, respectively, s.c., 4 h after S. cerevisiae injection) attenuated baker’s yeastinduced fever by 61.0% and 82.4%, respectively. These two effective antipyretics were selected to investigate the mechanisms of action. The effects on cyclooxygenase-1 and -2 (COX-1 and COX-2) activities, on 1,1-diphenyl-2-picrylhydrazyl (DPPH) oxidation in vitro, on TNF-a and IL- 1b levels and on leukocyte counts in the washes of peritoneal cavities of rats injected with baker’s yeast were determined. While 3ethyl- and 3propyl-TFDP did not reduce baker’s yeastinduced increases of IL-1 or TNF- levels, 3ethyl-TFDP caused a 42% reduction in peritoneal leukocyte count. 3ethyl- and 3propyl-TFDP did not alter COX-1 and COX-2 activities in vitro, but presented antioxidant activity in the DPPH assay with an IC50 of 39.3 (25.0-62.0) mM and 162.9 (135.6-195.7) mM, respectively. In a other set of the experiments, we investigate the effect of 3- ethyl- and 3-propyl-5-hydroxy-5-trifluoromethyl-4,5-dihydro-1H-1-carboxyamidepyrazoles on S.cerevisiae-induced peritoneal inflammation in rats. Pre-treatment with 3ethyl-TFDP (140 μmol/kg, 5 mL/Kg) significantly prevented S.cerevisiae-induced increase in leukocyte influx, peritoneal vascular permeability and myeloperoxidase activity, but had no effect on TNF-a and IL-1b levels. On the other hand, 3propyl-TFDP (200 μmol/kg, 5 mL/Kg) had no effect on these inflammatory parameters. The current study describes two novel antipyretic pyrazole derivatives, whose mechanisms of action do not involve the classic inhibition of the COX pathway or pyrogenic cytokine release. In addition, it is shown that 3ethyl-TFDP presents antiinflammatory potential, since it reduces leukocyte influx, peritoneal vascular permeability and MPO activity. Taken together, our data suggest that the pyrazole derivatives 3ethyl- and 3propyl-TFDP seems a promising antipyretic and anti-inflammatory compounds.
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Frigo, Leandro Marcon. "Obtenção de novos heterociclos derivados do ácido levulínico." Universidade Federal de Santa Maria, 2013. http://repositorio.ufsm.br/handle/1/4263.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico
This study describes the attainment of twenty three (23) bis-heterocycles derived from the Levulinic Acid: Bis-Pyrazoles (6a-k) by the reaction of cyclecondensation between the 3-(5-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-3-il)propanohidrazidamand a series of replaced β-alcoxiviniltrifluorometilcetonas. 1,3,4-oxadiazole 2-5-disubstituted (8-11) by reactions like [4 + 1] [OCNN+C], through the reactions of cyclecondensation between the 3-(5-(trifluoromethyl)-4,5-dihydro-1H-pyrazol-3-yl)propanohidrazida with different orthoesters as well as with carbon disulfide. It was also produced hydrazides (16c-d, g-h e 17c-d, g-h) derived of synthesized pyrimidines, to be used as precursorsn in the synthesis of bis-heterocycles, derivatizated of the reaction of those with some β- Ketones alcoxiviniltrifluormetil. The bis-heterocycles were obtained by the ordinary methodology, with efficiency between 61-97%.It was also gotten other original compounds (3i-k, 5), used as precursors in this study. The structure of these synthesized compounds were confirmed by the data of RMN 1H, 13C, besides the data of mass spectrometry.
Este trabalho descreve a obtenção de 23 novos bis-heterociclos derivados do Ácido Levulínico: Bis-Pirazóis (6a-k) a partir da reação de ciclocondensação entre o 3-(5-(trifluorometil)-4,5-dihidro-1H-pirazol-3-il)propanohidrazida e uma série de β-alcoxiviniltrifluorometilcetonas substituídas; 1,3,4-oxadiazóis 2-5-dissubstituídos (8-11) via reações do tipo [4 + 1] [OCNN+C], através de reações de ciclocondensação entre a 3-(5-(trifluorometil)-4,5-dihidro-1H-pirazol-3-il)propanohidrazida com diferentes ortoésteres, bem como com dissulfeto de carbono. Foram produzidas ainda, hidrazidas( 16c-d, g-h e 17c-d, g-h) derivadas de pirimidinas sintetizadas, para serem utilizadas como precursores na síntese de bis-heterociclos, derivatizados da reação destas com algumas β-alcoxiviniltrifluormetil cetonas. Os bis-heterociclos foram obtidos por metodologia convencional, com rendimentos entre 61-97%. Foram obtidos ainda outros compostos inéditos (3i-k, 5) utilizados como precursores nesse trabalho. As estruturas dos compostos sintetizados foram confirmadas por dados de RMN 1H, 13C, além de dados de espectrometria de massas.
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Friedein, Alynne Alegre Souto. "Síntese de novos azóis derivados da 1,1- difenilacetona." Universidade Federal de Santa Maria, 2014. http://repositorio.ufsm.br/handle/1/10591.

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This work describes an efficient method to obtaining new heterocycles from the reaction of acetalization of the ketonic carbonyl, followed by acylation of the enolether, generated in situ from the acetal derivative of 1,1-diphenylacetone, with trifluoroacetic anhydride, tricloroacetila of chloride, clorodiflúoracético anhydride, pentaflúorpropiônico anhydride in the absence of solvents. There were performed reactions of cyclocondensation between 1,1,1-trialo-4-alkoxy-3-alquen-2-ones and hydroxylamine hydrochloride, forming, in general, the 5-trialometil-5-hydroxy-4,5-diidroisoxazóis. To obtaining pyrazoline compounds, was proposed the cyclocondensation between the β-ketones alcoxivinil (ou é β-alcoxivinil ketones?) and four different dinucleophiles: monohydrate hydrazine, phenylhydrazine, thiosemicarbazide and aminoguanidine carbonate. All compounds synthesized on this work, since the acetal to the final heterocycles are inedited and their structures were confirmed by RMN 1H e 13C data. In this work, were also performed antimicrobial activity tests of some compounds against microorganisms, wherein some showed significant result for bacteria of great clinical interest, Staphylococcus aureus.
Este trabalho descreve um método eficiente para a obtenção de novos heterociclos a partir da reação de acetalização da carbonila cetônica, seguida pela acilação do enoléter, gerado in situ a partir do acetal derivado da 1,1-difenilacetona, com anidrido trifluoracético, cloreto de tricloroacetila, anidrido clorodiflúoracético e anidrido pentaflúorpropiônico na ausência de solventes. Foram realizadas reações de ciclocondensação entre as 1,1,1-trialo-4-alcoxi-3-alquen-2-onas e cloridrato de hidroxilamina, formando, de maneira geral, os 5-trialometil-5-hidroxi-4,5-diidroisoxazóis. Para obtenção dos compostos pirazolínicos, foi proposta a ciclocondensação entre as β-alcoxivinil cetonas e quatro diferentes dinucleófilos: monohidrato de hidrazina, fenilhidrazina, tiosemicarbazida e carbonato de aminoguanidina. Todos os compostos sintetizados neste trabalho, desde o acetal até os heterociclos finais são inéditos e suas estruturas foram confirmadas por dados de RMN 1H e 13C. Neste trabalho, também foram realizados testes de atividade antimicrobiana de alguns compostos contra microorganismos, sendo que alguns apresentaram significativo resultado para a bactéria de grande interesse clínico, Staphylococcus aureus.
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Books on the topic "Pyrazole derivates"

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Wiley, Richard H., and Paul F. Wiley. Pyrazolones, Pyrazolidones, and Derivatives. Wiley & Sons, Incorporated, John, 2009.

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Book chapters on the topic "Pyrazole derivates"

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Niedenzu, Kurt, and Swiatoslaw Trofimenko. "Pyrazole derivatives of boron." In Topics in Current Chemistry, 1–37. Berlin, Heidelberg: Springer Berlin Heidelberg, 1986. http://dx.doi.org/10.1007/3-540-15811-1_1.

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Fustero, Santos, Juan F. Sanz-Cervera, Antonio Simón-Fuentes, Raquel Román, Silvia Catalán, and Marcelo Murguía. "New Fluorinated Pyrazol and Uracil Derivatives: Synthesis and Biological Activity." In ACS Symposium Series, 182–209. Washington, DC: American Chemical Society, 2009. http://dx.doi.org/10.1021/bk-2009-1003.ch009.

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Swarts, Steven G., Mei Zhang, Liangjie Yin, Chaomei Liu, Yeping Tian, Yongbing Cao, Michael Swarts, et al. "Antioxidant Properties of Select Radiation Mitigators Based on Semicarbazone and Pyrazole Derivatives of Curcumin." In Oxygen Transport to Tissue XXXII, 291–97. Boston, MA: Springer US, 2011. http://dx.doi.org/10.1007/978-1-4419-7756-4_39.

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Emandi, A., M. Calinescu, S. Ioachim, R. Georgescu, and I. Serban. "Synthesis and Characterization of the 2:1 Copper(II) Complexes With 4-Arylazo-Pyrazol-5-One Derivatives." In Multiphoton and Light Driven Multielectron Processes in Organics: New Phenomena, Materials and Applications, 489–502. Dordrecht: Springer Netherlands, 2000. http://dx.doi.org/10.1007/978-94-011-4056-0_36.

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Caravatti, G., J. Brüggen, E. Buchdunger, R. Cozens, P. Furet, N. Lydon, T. O'Reilly, and P. Traxler. "Pyrrolo[2,3-d]pyrimidine and Pyrazolo[3,4-d]pyrimidine Derivatives as Selective Inhibitors of the EGF Receptor Tyrosine Kinase." In Anticancer Agents, 231–44. Washington, DC: American Chemical Society, 2001. http://dx.doi.org/10.1021/bk-2001-0796.ch014.

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Angulwar, Jaman A. "Multicomponent Synthesis of 2-Substituted Derivatives of 6-Amino-5-Cyano-1,4-Dihydro-3-Methyl-1,4-Diphenylpyrano-[2,3-C]-Pyrazole Using Knoevenagel and Michael Addition." In Modern Green Chemistry and Heterocyclic Compounds, 113–36. Series statement: Innovations in physical chemistry: monographic series: Apple Academic Press, 2020. http://dx.doi.org/10.1201/9780367276942-4.

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Ambhore, Ajay N. "An Efficient Green Synthesis of Diphenyl Pyrazol-4-Yl-Thiopyridin-4-Yl-1,3,4-Oxadiazole Derivatives and Evaluation of Their Antimicrobial and Antioxidant Activity." In Modern Green Chemistry and Heterocyclic Compounds, 79–111. Series statement: Innovations in physical chemistry: monographic series: Apple Academic Press, 2020. http://dx.doi.org/10.1201/9780367276942-3.

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Taber, Douglass. "Preparation of Heteroaromatic Derivatives." In Organic Synthesis. Oxford University Press, 2011. http://dx.doi.org/10.1093/oso/9780199764549.003.0067.

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Several new routes to furans and to pyrroles have recently been put forward. Inspired by the Achmatowicz ring expansion, Patrick J. Walsh of the University of Pennsylvania developed (J. Am. Chem. Soc. 2008, 130, 4097) the oxidative rearrangement of 3-hydrox-alkyl furans such as 1 to the 3-aldehyde 2. José M. Aurrecoechea of the Universidad del País Vasco established (J. Org. Chem. 2008, 73, 3650) that cumulated alcohols, available by reduction of alkynes such as 3 with SmI2, rearrange under Pd catalysis, and then add to an acceptor alkene such as 4, to give the furan 5. Vladimir Gevorgyan of the University of Illinois at Chicago used (J. Am. Chem. Soc. 2008, 130, 1440) an Au catalyst to rearrange an allene such as 6 to the bromo furan 7. Fabien L. Gagosz of the Ecole Polytechnique, Palaiseau, also found (Organic Lett. 2007, 9, 3181) that an Au catalyst rearranged the eneyne 8 to the pyrrole 9. Azido esters such as 10 are readily prepared from the corresponding aldehyde by phosphonate condensation. Shunsuke Chiba and Koichi Narasaka of Nanyang Technology University demonstrated (Organic Lett. 2008, 10, 313) that thermal condensation of 10 with acetyl acetone 11 gave the pyrrole 12, while Cu catalyzed condensation with acetoacetate 13 gave the complementary pyrrole 14. Huan-Feng Jiang of South China University of Technology observed (Tetrahedron Lett. 2008, 49, 3805) that condensation of an acid chloride 15 with an alkyne 16, presumably to give the alkynyl ketone, followed by the addition of hydrazine delivered the pyrazole 17. Masanobu Uchiyama of RIKEN and Florence Mongin of the Université de Rennes 1 established (J. Org. Chem. 2008, 73, 177) that a pre-formed pyrazole 18 could be metalated and then iodinated, to give 19. Xiaohu Deng of Johnson & Johnson, San Diego reported (Organic Lett. 2008, 10, 1307; J. Org. Chem. 2008, 73, 2412) complementary routes to pyrazoles, combining 20 and 21 under acidic conditions to give 22, and under basic conditions to give 23.
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"Pyrazine Derivatives as Green Corrosion Inhibitors." In Theory and Applications of Green Corrosion Inhibitors, 161–82. Materials Research Forum LLC, 2021. http://dx.doi.org/10.21741/9781644901052-6.

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Pyrazine is a six-member heterocyclic compound containing two nitrogen atoms, located at one-fourth position. A pyrazine and its derivatives are most commonly used as a pharmaceutical, food colouring agent and as a corrosion inhibitor. It has chemistry and chemical characteristics due to nitrogen atoms present which can be obtained from both naturally and synthetically. A pyrazine and its derivatives are used effectively in corrosion media to prevent metal and metal alloy from corrosion. Chemical and electrochemical methods are commonly used as corrosion monitoring techniques, in which weight loss EIS and PDP are prominent. Their mixed type of nature has been reported in previously published works. There have also been works on the use of computation calculation in recent works, which include DFT calculation and MD Simulation are the main ones. The future research related to the pyrazine has also been highlighted.
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Grimmett, M. R. "Photolysis of Pyrazine Derivatives." In Five-Membered Hetarenes with Two Nitrogen or Phosphorus Atoms, 1. Georg Thieme Verlag KG, 2002. http://dx.doi.org/10.1055/sos-sd-012-00545.

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Conference papers on the topic "Pyrazole derivates"

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Gondek, E., J. Niziol, A. Danel, and J. Sanetra. "Photovoltaic effect based on pyrazole derivatives." In 2009 3rd ICTON Mediterranean Winter Conference (ICTON-MW 2009). IEEE, 2009. http://dx.doi.org/10.1109/ictonmw.2009.5385546.

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Liu, Xiaobo, Shan Xu, and Yinhua Xiong. "Synthesis of 3-phenyl-1H-pyrazole Derivatives." In 2016 7th International Conference on Education, Management, Computer and Medicine (EMCM 2016). Paris, France: Atlantis Press, 2017. http://dx.doi.org/10.2991/emcm-16.2017.117.

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Priyanka, S., S. Sivapriya, D. Sivakumar, M. Gopalakrishnan, M. Seenivasan, and H. Manikandan. "Synthesis and DFT calculation of novel pyrazole derivatives." In INTERNATIONAL CONFERENCE ON RECENT TRENDS IN APPLIED MATHEMATICAL SCIENCES (ICRTAMS-2020). AIP Publishing, 2021. http://dx.doi.org/10.1063/5.0063016.

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Oumessaoud, Asmaa, Jamila Bouali, Salha Hamri, Hajiba Ouchetto, Abderrafia Hafid, Mostafa Khouili, and Maria Dolors Pujol. "Efficient Synthesis of New Pyrazoles Derivatives via Functionalized Aryl-Sydnones." In 1st International Electronic Conference on Catalysis Sciences. Basel, Switzerland: MDPI, 2020. http://dx.doi.org/10.3390/eccs2020-07565.

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Ali, Tarik, Somaia Abdel-Karim, Kamilia El-Mahdy, and Salah Abdel-Aziz. "Synthesis and antimicrobial activities of some novel bis-pyrazole derivatives containing a hydrophosphoryl unit." In The 14th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2010. http://dx.doi.org/10.3390/ecsoc-14-00374.

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talbi, soumaya, souad rabi, hafid Abderrafia, and mostafa khouili. "Efficient Synthesis of Pyrazolo-Enaminone Derivatives and Evaluation of Their Biological Activities." In 1st International Electronic Conference on Catalysis Sciences. Basel, Switzerland: MDPI, 2020. http://dx.doi.org/10.3390/eccs2020-07540.

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Трофимов, Б., B. Trofimov, Н. Гусарова, and N. Gusarova. "The development of original methodologies of directed synthesis of le-Carbs their analogs and precursors base donacetylene and its derivatives." In Topical issues of translational medicine: a collection of articles dedicated to the 5th anniversary of the day The creation of a department for biomedical research and technology of the Irkutsk Scientific Center Siberian Branch of RAS. Москва: INFRA-M Academic Publishing LLC., 2017. http://dx.doi.org/10.12737/conferencearticle_58be81ec92d17.

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New reactions, which have been discovered and continue to be developed in A.E. Favorsky Irkutsk institute of chemistry SB RAS on the basis of acetylene, a product of oil, gas and coal processing and multi-faceted building block for organic synthesis, have been considered. These reactions provide for the shortest routes to construction of fundamental heterocyclic scaffolds (pyrroles, imidazoles, pyrazoles, indoles, pyridines, dihydropyridines, etc.) with desirable and optimum combination of functional pharmacophoric groups and fragments, which are responsible for antiviral (HIV, flu), antitumor, tuberculostatic and hypotensive activities.
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Li, Yan, and Xiao-Shuang Ma. "Optical properties of pyrazine derivatives compared with their s-triazine analogs." In 6th International Conference on Mechatronics, Materials, Biotechnology and Environment (ICMMBE 2016). Paris, France: Atlantis Press, 2016. http://dx.doi.org/10.2991/icmmbe-16.2016.23.

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Shukla, Bindesh Kumar, and Umesh Yadava. "QSAR study of some pyrazolo[3,4-d]pyrimidine derivatives as the c-Src inhibitors." In INTERNATIONAL CONFERENCE ON CONDENSED MATTER AND APPLIED PHYSICS (ICC 2015): Proceeding of International Conference on Condensed Matter and Applied Physics. Author(s), 2016. http://dx.doi.org/10.1063/1.4946371.

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Jachak, Madhukar, Naresh Badgujar, and Nilambari Yewalkar. "Reactions of 5-aminopyrazole with Active Methylene Compounds:Synthesis of Pyrazolo[3,4-b]pyridine Derivatives." In The 9th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2005. http://dx.doi.org/10.3390/ecsoc-9-01463.

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