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Journal articles on the topic 'Pyrazole derivatives'

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Published: 4 June 2021

Last updated: 26 July 2025

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1

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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2

M., K. A. IBRAHIM, H. H. ELGHANDOUR A., S.M. ABDBL-SAYED G., and S.M. ABDEL FATTAH A. "Synthesis of Pyrazoles and Fused Pyrazoles. Novel Synthesis of Pyrano[2,3-c]pyrazole, Thieno[2,3-c]pyrazole and Pyrazolo[3,4-b ]pyridine Derivatives." Journal of Indian Chemical Society Vol. 74, Mar 1997 (1997): 206–8. https://doi.org/10.5281/zenodo.5885902.

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Department of Chemistry, Faculty of Science, Cairo University, Giza, A. R. Egypt <em>Manuscript received 17 November 1994, revised 26 July 1995, accepted 28 September 1995</em> 3-Metbyl-1-thiocarbamoylpyrazoi-5-one (1) reacted with <em>p</em>-metbylpbenscyl bromide to give 3-metbyl-1(4-tbiazol-2-yl)pyrazol-5-one (2). Compounds 1 and 2 were reacted with reagents such as α-cyanocinnamo. benzaldehyde, elemental suJphurlmalononltrlle, benzenediazomum chloride, pyrazol-5-yl-diazonium chloride malononitriie, and ethyl acetoacetate to afford pyrano[2,3-<em>c</em>]pyrazoles (4, 6) Pyra

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3

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 (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, arylid

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4

Farooq, Saba, and Zainab Ngaini. "Chalcone Derived Pyrazole Synthesis via One-pot and Two-pot Strategies." Current Organic Chemistry 24, no. 13 (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., pyraz

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5

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 exp

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6

Lerner, Hans-Wolfram, Günter Margraf, Tonia Kretz, et al. "Redox Behaviour of Pyrazolyl-Substituted 1,4-Dihydroxyarenes: Formation of the Corresponding Semiquinones, Quinhydrones and Quinones." Zeitschrift für Naturforschung B 61, no. 3 (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 gr

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7

Alsayari, Abdulrhman, Abdullatif Bin Muhsinah, Yahya I. Asiri, et al. "Arylhydrazono/Aryldiazenyl Pyrazoles: Green One-Pot Solvent-Free Synthesis and Anticancer Evaluation." Letters in Organic Chemistry 17, no. 10 (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, s

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8

Farag, Awatef A., Mohamed F. El Shehry, Samir Y. Abbas, et al. "Synthesis of pyrazoles containing benzofuran and trifluoromethyl moieties as possible anti-inflammatory and analgesic agents." Zeitschrift für Naturforschung B 70, no. 7 (2015): 519–26. http://dx.doi.org/10.1515/znb-2015-0009.

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AbstractSearching for new anti-inflammatory and analgesic agents, we have prepared a series of novel pyrazoles containing benzofuran and trifluoromethyl moieties. The pyrazole derivatives have been synthesized via two routes starting from 5-(3-(trifluoromethyl)phenyl azo) salicylaldehyde. The first route involved the synthesis of 2-acetylbenzofuran and then treatment with aldehydes to afford the corresponding chalcones. The cyclization of the latter chalcones with hydrazine hydrate led to the formation of new pyrazoline derivatives. The second route involved the synthesis of benzofuran-2-carbo

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9

Hrynyshyn, Yevhenii, Hanna Musiichuk, Olena Komarovska-Porokhnyavets, et al. "Synthesis and Antimicrobial Activity of 4-Arylthio- and 4 Alkylthiofunctionalized Pyrazolo[1,5-a]pyrazines." Ukrainian Chemistry Journal 85, no. 1 (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 dimethyl

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10

M., K. A. IBRAHIM, H. H. ELGHANDOUR A., ABOU-HADEED K., and S. ABDELHAFIZ I. "Utility of Hydrazidoyl Chlorides : Synthesis of New Pyrazoles, Pyrazolo[ 3,4-d]pyridazines, Pyrazolo[4,5-b]pyridines and Pyrazolo[ 4,5-d]pyrimidine Derivatives." Journal of Indian Chemical Society Vol. 69, Jul 1992 (1992): 378–80. https://doi.org/10.5281/zenodo.6004337.

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Chemistry Department, Faculty of Science, Cairo University, Giza, Egypt Chemistry Department, Faculty of Science. Suez-Canal University, Ismalia, Egypt <em>Manuscript received 28 October 1991 revised 26 May 1992, accepted 3 June 1992</em> Hydrazidoyl chlorides (1) were reacted with a variety of active methylene compounds and arylidemnialononitriles .1 medium, to produce polyfunctionally substituted pyrazole derivatives (2-6 and 10). The pyrazoles (2, 3, 6 and 10) were converted into the corresponding pyrazolo[3, 4-<em>d</em>]pyridazine derivatives (7 - 9 and 14), respectively. The aminopyraiol

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11

Erdem, Ahmet, Hasan Genc, Nejdet Sen, Rafet Kilincarslan, and Emin Erdem. "The Synthesis and Reactions of Novel Pyrazole Derivatives by 4-phenylcarbonyl-5-phenyl-2,3-dihydro-2,3-furandione Reacted with Some Hydrazones." Revista de Chimie 68, no. 1 (2017): 143–46. http://dx.doi.org/10.37358/rc.17.1.5407.

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We report some novel pyrazole derivatives taking 4-phenylcarbonyl-5-phenyl-2,3-dihydro-2,3-furandione, 1. For this, 4-phenylcarbonyl-5-phenyl-2,3-dihydro-2,3-furandione, 1 was reacted with benzaldehyde(2- or 4-fluorophenyl)hydrazone to give 4-benzoyl-1-(2- or 4-fluorophenyl)-5-phenyl-1H-pyrazole-3-carboxylic acid 2a,b. Pyrazol derivative containing 2-fluorophenyl group 2a was converted into carboxylic chloride derivative 3a by thionyl chloride and then the compound 4a was obtained from reaction ammonia with compound 3a. In the next step, 4-benzoyl-1-(2-fluorophenyl)-5-phenyl-1H-pyrazole-3-carb

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12

Rizk, Sameh, Ismail M. Awheda, and Fathi A. Smida. "Synthesis and DFT Study of Newly Schiff Base and Fused Heterocyclic Compounds as Antibacterial Agent." JOURNAL OF ADVANCES IN CHEMISTRY 16 (November 7, 2019): 5395–403. http://dx.doi.org/10.24297/jac.v16i0.8499.

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Treatment of 2,3-di-(4-chlorophenyl) oxirane-2,3-dicarbonitriles(1) with nitrogen nucleophiles, e.g. N2H4, NH2OH afforded pyrazole 2, 1.2oxazole 3 derivatives respectively The 3-amino pyrazole-4-one derivatives 2 can be used as a key starting materials to synthesize some important Schiff base 4 and fused heterocyclic compounds e.g. Imidazolo-[4,5-c]pyrazole 5, Pyrazolo[3,4-e]1,2,4-triazine 6, pyrazol[1,2-a] 1,3,5-triazine 7, 8 and 9. The electromeric effect of the halogen atom in the aryl moieties can be controlled upon the rate of reaction and the yield of the product. The structures of synth

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13

Queiroz, Jaqueline E., Lucas D. Dias, Giuliana M. Vila Verde, Gilberto L. B. Aquino, and Ademir J. Camargo. "An Update on the Synthesis and Pharmacological Properties of Pyrazoles Obtained from Chalcone." Current Organic Chemistry 26, no. 2 (2022): 81–90. http://dx.doi.org/10.2174/1385272826666220119110347.

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Abstract: A review concerning the synthesis and pharmacological properties of pyrazoles obtained from Chalcone described in the literature over the last 5 years (2016-2020) was presented and discussed. Among the synthetic approaches for pyrazoles described so far, the cyclization and acetylation method of α,β-unsaturated chalcones, and substituted hydrazine were selected and analyzed. 105 pyrazole derivatives (3-107) were evaluated as well as their pharmacological activities, namely, antineoplastic, anti-inflammatory, antioxidant, antibacterial, antifungal, antimycobacterial, antiplasmodial, A

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14

Thirunarayanan, Ganesamoorthy, and K. Ravi. "Synthesis and Spectral Correlation Study of some 3-(3,4-dichlorophenyl)-5-(Substituted Phenyl)-4,5-dihydro-¹H-Pyrazole-1-yl-Ethanones." International Letters of Chemistry, Physics and Astronomy 19 (October 2013): 44–57. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.19.44.

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Some N-acetyl pyrazoles including 3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazole-1-yl-ethanones have been synthesised by solvent free cyclization cum acetylation of chalcones including substituted styryl 3,4-dichlorophenyl ketones using hydrazine hydrate and acetic anhydride in presence of catalytic amount of fly-ash: H2SO4 catalyst. The yield of these N-acetyl pyrazole derivatives are more than 75%. The synthesised N-acetyl pyrazoline derivatives were characterized by their physical constants and spectral data. The infrared spectral νC=N and C=O (cm-1) frequencies, NMR

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15

Thirunarayanan, Ganesamoorthy, and K. Ravi. "Synthesis and Spectral Correlation Study of some 3-(3,4-dichlorophenyl)-5-(Substituted Phenyl)-4,5-dihydro-<sup>1</sup><i>H</i>-Pyrazole-1-yl-Ethanones." International Letters of Chemistry, Physics and Astronomy 19 (October 2, 2013): 44–57. http://dx.doi.org/10.56431/p-7i78p0.

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Some N-acetyl pyrazoles including 3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazole-1-yl-ethanones have been synthesised by solvent free cyclization cum acetylation of chalcones including substituted styryl 3,4-dichlorophenyl ketones using hydrazine hydrate and acetic anhydride in presence of catalytic amount of fly-ash: H2SO4 catalyst. The yield of these N-acetyl pyrazole derivatives are more than 75%. The synthesised N-acetyl pyrazoline derivatives were characterized by their physical constants and spectral data. The infrared spectral νC=N and C=O (cm-1) frequencies, NMR

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16

Milišiūnaitė, Vaida, Rūta Paulavičiūtė, Eglė Arbačiauskienė, Vytas Martynaitis, Wolfgang Holzer, and Algirdas Šačkus. "Synthesis of 2H-furo[2,3-c]pyrazole ring systems through silver(I) ion-mediated ring-closure reaction." Beilstein Journal of Organic Chemistry 15 (March 14, 2019): 679–84. http://dx.doi.org/10.3762/bjoc.15.62.

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Fused pyrazole ring systems are common structural motifs of numerous pharmaceutically important compounds. Nevertheless, access to derivatives of the aromatic 2H-furo[2,3-c]pyrazole ring system is still quite limited, and their chemistry and functional properties remain largely underexplored. The current study investigates routes to construct this system from easily accessible starting materials using metal-catalyzed reactions. A simple and efficient procedure to access the 2H-furo[2,3-c]pyrazole ring system was developed by employing the silver(I) ion-mediated ring-closure reaction of 4-alkyn

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17

Albar, Hassan A. "1,3-Dipolar Cycloaddition of Four Hydrazonoyl Chlorides to β-Diketones and α,β-Unsaturated Ketones". Journal of Chemical Research 23, № 3 (1999): 182–83. http://dx.doi.org/10.1177/174751989902300306.

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The 1,3-dipolar cycloaddition of four hydrazonoyl chloride derivatives with the sodium salt of unsymmetrical β-diketones (benzoylacetone) offers a versatile method for the regioselective synthesis of 2 H-pyrazoles in a similar fashion to the cycloaddition of the nitrilimides with α,β-unsaturated ketones and esters; the structures of the prepared isomeric pyrazole and pyrazoline derivatives are established by spectroscopic and chemical methods.

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18

Edrees, Mastoura M. "Synthesis of 4-hydrazinopyrazolo[3,4-d]pyrimidines and their Reactions with Carbonyl Compounds." Journal of Chemical Research 37, no. 1 (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

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19

M., K. A. IBRAHIM, M. EL-REEDY A., S. EL-GHARIE M., and M. FARAG A. "Activated Nitrile in Heterocyclic Synthesis. A Novel Synthesis of Pyrazolo[3,4-b]pyridine, Pyrrolo[2, 3 -c ]pyrazole, Pyrano[2,-3c ]pyrazole and Pyrrolo[3,4-c ]pyrazole." Journal of Indian Chemical Society Vol. 64, Jun 1987 (1987): 345–47. https://doi.org/10.5281/zenodo.6237953.

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Chemistry Department, Faculty of Science, Cairo University, Giza, A. R. Egypt <em>Manuscript received 14 Match 1986, revised 4 November 1986, accepted 22 April 1987</em> The hydrazidoyl halides (2a — c) react with 2- amino-l,1,3-tricyano-1-propene (1a), diethyl 3-amino-2-cyano-2-pentene-1,5-dicarboxylate (1b), 3-iminobutaronitrile (1c), succinonitrile, 1,3 dicyano-2-iminopropane and 1,3-dicyanoacetone in sodium ethoxide solution to give the corresponding pyrazolo[3,4-<em>b</em>]pyridine (6), pyrano[2,3-<em>c</em>]pyrazole (7), pyrazole (10), pyrrolo[2,3-<em>c</em>]pyrazole (11), pyrazolo

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20

I.H. El-Qaliei, Mohamed, Sayed A.S. Mousa, Esam A. Ishak, Hamdi M.D. Nasr, Modather F Hussein, and Abdallah M.A. Hassane. "Synthesis, characterization, antimicrobial, antioxidant activities, and in silico study of new azo disperse dyes containing pyrazole and pyrazolo[1,5-a]pyrimidine rings." Bulletin of the Chemical Society of Ethiopia 39, no. 7 (2025): 1411–24. https://doi.org/10.4314/bcse.v39i7.13.

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New N,N-dimethyl-N'-(5-oxo-4-(aryldiazenyl)-2,5-dihydro-1H-pyrazol-3-yl)formimidamide 5a-c are formed by reaction of 5-amino-1H-pyrazol-3(2H)-one derivatives 4a-c with N,N-dimethylformamide dimethyl acetal (DMF-DMA). Compounds 5a-c serve as excellent precursors for the synthesis of new disazo pyrazole disperse dyes, When refluxed with hydrazine hydrate or active methylene reagents 8a,b, leading to N''-(3-hydroxy-4-(arylaza)-1H-pyrazol-5-yl)formimidohydrazide 7a-c or pyrazolo[1,5-a]. pyrimidines 11a–e. In vitro studies were carried out to evaluate antioxidant properties of the produced compound

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21

Shaikh, Sabiya K.* Md. Rayees Ahemad. "Review: Anticancer Activity Of Pyrazole." International Journal in Pharmaceutical Sciences 2, no. 3 (2024): 334–40. https://doi.org/10.5281/zenodo.10809286.

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The study of pharmaceutical chemistry is devoted to the search for and development of novel therapeutic medicines. While inorganic substances like antacids, mineral supplements, and radiopharmaceuticals continue to play a significant role in therapy, organic molecules with more focused pharmacological actions are gaining ground. The five and six-membered heterocyclic nitrogen-containing systems, which have demonstrated their effectiveness in fields like anti-bacterial, fungicidal, anti-inflammatory, anticonvulsant, diuretics, and anti-histaminic treatments, are among the most significant in on

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22

El-Telbani, Emad M., Ibrahim Radini, and Sameh R. Elgogary. "Syntheses of tricyclic fused quinoxaline ring systems: Pyrazoloquinoxalines (a-review)." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 02 (2025): 279. https://doi.org/10.59467/ijhc.2025.35.279.

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Quinoxaline derivatives have gained significant interest due to their diverse pharmacological activity and have been included in numerous marketed drugs used to treat of various diseases. Examples include glecaprevir (Mavyret), voxilaprevir (Vosevi), Balversa (L01EX16) (erdafitinib), carbadox, XK469R (NSC698215), and becampanel (AMP397). Among the five-membered fused tricyclic quinoxalines ring systems, the pyrazoloquinolines belong to the azaheterocyclic group as derivatives of quinoxalines and pyrazoles and have characterized by many biological and pharmaceutical properties. There are three

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23

Ebenezer, Oluwakemi, Michael Shapi, and Jack A. Tuszynski. "A Review of the Recent Development in the Synthesis and Biological Evaluations of Pyrazole Derivatives." Biomedicines 10, no. 5 (2022): 1124. http://dx.doi.org/10.3390/biomedicines10051124.

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Pyrazoles are five-membered heterocyclic compounds that contain nitrogen. They are an important class of compounds for drug development; thus, they have attracted much attention. In the meantime, pyrazole derivatives have been synthesized as target structures and have demonstrated numerous biological activities such as antituberculosis, antimicrobial, antifungal, and anti-inflammatory. This review summarizes the results of published research on pyrazole derivatives synthesis and biological activities. The published research works on pyrazole derivatives synthesis and biological activities betw

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24

Zang, Binbin, та Lihui Wang. "Synthesis and protective effect of pyrazole conjugated imidazo[1,2-a]pyrazine derivatives against acute lung injury in sepsis rats via attenuation of NF-κB, oxidative stress, and apoptosis". Acta Pharmaceutica 73, № 3 (2023): 341–62. http://dx.doi.org/10.2478/acph-2023-0031.

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Abstract The current work was conducted to elucidate the pharmacological effect of pyrazole-conjugated imidazo[1,2-a]pyrazine derivatives against acute lung injury in rats in sepsis and their mechanism of action. Various pyrazole-conjugated imidazo[1,2-a]-pyrazine derivatives have been synthesized in a straightforward synthetic route. They exhibited a diverse range of inhibitory activity against NF-ĸB with IC 50 ranging from 1 to 94 µmol L–1. Among them, compound 3h [(4-(4-((4-hydroxyphenyl)sulfonyl) phenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl) (8-(methylamino)imidazo[1,2-a]pyrazin

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25

Hosny, Mona A., Yasser H. Zaki, Wafaa A. Mokbel, and Abdou O. Abdelhamid. "Synthesis, Characterization, Antimicrobial Activity and Anticancer of Some New Pyrazolo[1,5-a]pyrimidines and Pyrazolo[5,1-c]1,2,4-triazines." Medicinal Chemistry 16, no. 6 (2020): 750–60. http://dx.doi.org/10.2174/1573406415666190620144404.

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Background: Pyrazole and its derivatives are known to exhibit significant biological and pharmacological activities such as anticancer, anti-inflammatory, antioxidant, antibacterial, analgesic, antiviral, antimicrobial, antifungal, anti-glycemic, antiamoebic, and antidepressive. Considering the immense biological properties, pyrazole is one of the most widely studied nitrogen- containing heterocyclic nuclei. Fused pyrazole derivatives are composed of the pyrazole nucleus attached to other heterocyclic moieties. Objective: The objective of this article is the synthesis of some new pyrazolo[1,5-

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26

A, Kumar Maddineni, Rao Chunduri V, and Raju Begari N. "Synthesis and Characterization of Novel Mono Carbonyl Curcumin Analogues of Pyrazole Derivatives." Der Pharma Chemica 13, no. 1 (2021): 6. https://doi.org/10.5281/zenodo.13644078.

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(E)-4-aryl-1-phenyl-1H-pyrazol-4-yl)but-3-en-2-one derivatives were (4a-d) synthesized by the condensation of 3-aryl-1-phenyl-1H-pyrazole-4- carbaldehyde derivatives (3a-d) with acetone in the presence of sodium hydroxide. Compounds (4a-d) on condensation with different aldehydes give mono carbonyl curcumin analogues (MACs) of pyrazole derivatives (6a-x) in good yield.

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27

Lamie, Phoebe F. "Synthesis and Antimicrobial Activity of some Novel Isoindoline-1,3-Dione Derivatives." JOURNAL OF ADVANCES IN CHEMISTRY 8, no. 2 (2008): 1660–66. http://dx.doi.org/10.24297/jac.v8i2.5570.

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New phthalimido derivatives incorporated with chalcone, pyrazole, pyrazoline, and pyrimidine moieties were synthesized and evaluated for their antimicrobial activities against bacterial and fungal strains. 2-{4-[1-Acetyl-5-(4-chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl} isoindoline-1,3-dione (7) showed broad spectrum antibacterial activity against both G+ and G- bacteria. While, (E)-2-{4-[3-(4-chlorophenyl)acryloyl]phenyl}isoindoline-1,3-dione (4b) showed promising antifungal activity.

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28

Çetin, Adnan, Ishak Bildirici, and Selçuk Gümüş. "Novel Pyrazole Derivatives Having Mono/Di Chiral Centered Group as Organocatalyst for Henry Reaction." Macedonian Journal of Chemistry and Chemical Engineering 39, no. 1 (2020): 17. http://dx.doi.org/10.20450/mjcce.2020.1954.

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The chiral substituted pyrazole-3-carboxamides (4a-c), pyrazole-3-carboxylates (5a-c), pyrazole-3-thioureides (7a-c) and pyrazole-3,4-dicarboxamides (10a-c) were prepared via the pyrazolo-3-chlorocarbonyl 2, pyrazolo-3,4-dicarboxy methyl ester 3 with pyrazole-3-isothiocyanate 6 with different (R)-chiral amino alcohols. All of the synthesized chiral compounds binding a pyrazole skeleton were investigated as organocatalysts for asymmetric aldol reactions between nitromethane and p-nitrobenzaldehyde in the presence of CuCl. Enantiomeric excesses and the reaction yields were found to be appropriat

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Ameziane El Hassani, Issam, Khouloud Rouzi, Hamza Assila, Khalid Karrouchi, and M’hammed Ansar. "Recent Advances in the Synthesis of Pyrazole Derivatives: A Review." Reactions 4, no. 3 (2023): 478–504. http://dx.doi.org/10.3390/reactions4030029.

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Pyrazole, characterized by a five-membered heterocyclic structure featuring two neighboring nitrogen atoms, serves as a core element. Pyrazoles hold a privileged status as versatile frameworks in various sectors of the chemical industry, including medicine and agriculture. Previous reviews have extensively highlighted the significance of pyrazoles and their diverse biological activities, encompassing roles such as antituberculosis, antimicrobial, antifungal, anti-inflammatory, anticancer, and antidiabetic agents. Consequently, they have garnered substantial interest from researchers. The aim o

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Kumar, Munish, and Sharad Kumar Panday. "Pyrazole and Its Derivatives: An Excellent N-Hetrocycle with Wide Range of Biological Applications (A Review)." Oriental Journal Of Chemistry 38, no. 3 (2022): 568–92. http://dx.doi.org/10.13005/ojc/380306.

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The pyrazole derivatives have been recognized as a unique heterocyclic molecule exerting broad range of biological activities such as analgesic, anti-viral, anti-histaminic, anti-microbial, anti-tumor, insecticides fungicides, anti-depressant, antipyretic, anti-inflammatory, angiotensin converting enzyme (ACE) inhibitory and estrogen receptor (ER) ligand activity etc. Pyrazoles also find applications in agrochemical and pharmaceutical industry. Pyrazoles have different chemical properties which may be attributed due to the effect of particular N-atoms present in pyrazole molecule. N-Atom prese

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Lusardi, Matteo, Maria Grazia Signorello, Eleonora Russo, et al. "Structure–Activity Relationship Studies on Highly Functionalized Pyrazole Hydrazones and Amides as Antiproliferative and Antioxidant Agents." International Journal of Molecular Sciences 25, no. 9 (2024): 4607. http://dx.doi.org/10.3390/ijms25094607.

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Aminopyrazoles represent interesting structures in medicinal chemistry, and several derivatives showed biological activity in different therapeutic areas. Previously reported 5-aminopyrazolyl acylhydrazones and amides showed relevant antioxidant and anti-inflammatory activities. To further extend the structure–activity relationships in this class of derivatives, a novel series of pyrazolyl acylhydrazones and amides was designed and prepared through a divergent approach. The novel compounds shared the phenylamino pyrazole nucleus that was differently decorated at positions 1, 3, and 4. The anti

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El-Naggar, Mohamed, Amira S. Abd El-All, Shweekar I. A. El-Naem, Mohamed M. Abdalla та Huda R. M. Rashdan. "New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative". Molecules 25, № 3 (2020): 672. http://dx.doi.org/10.3390/molecules25030672.

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This work describes the utility of pyrazole-4-carbaldehyde 1 as starting material for the synthesis of a novel potent series of 5α-reductase and aromatase inhibitors derived from 1,2,3-triazole derivative. Condensation of 1 with active methylene and different amino pyrazoles produced the respective Schiff bases 2–4, 8 and 9. On the other hand, 1 was reacted with ethyl cyanoacetate and thiourea in one-pot reaction to afford the pyrazolo-6- thioxopyridin-2-[3H]-one (10). Moreover, α–β unsaturated chalcone derivative 11 was prepared via the reaction of compound 1 with P-methoxy acetophenone, whic

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Abeed, Ahmed A. O., Talaat I. El-Emary, and Mohamed S. K. Youssef. "A Facile Synthesis and Reactions of Some Novel Pyrazole-based Heterocycles." Current Organic Synthesis 16, no. 3 (2019): 405–12. http://dx.doi.org/10.2174/1570179416666181210160908.

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<p>Aim and Objective: This work presents the synthetic capability and the exploitation of 1,3-diphenyl- 1H-pyrazole-4-carboxladehyde 1 and 5-diphenyl pyrazolyl-2-pyrazoline analogue 8 to serve as excellent precursors for the synthesis of substituted indol-2,3-dione, trizolo[3,4-a]benzazoles, thiazolo[2,3- a]benzimidazole-3-one, substituted 2-pyrazoline and pyrazole-substituted-pyrazolines using various reagents. </P><P> Materials and Methods: Using chemicals from Aldrich, Fluka, or Merck, and pure solvents, we apply the synthetic procedures for the synthesis of novel heterocy

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Kumar, Harish, Kushal Kumar Bansal, and Anju Goyal. "Synthetic Methods and Antimicrobial Perspective of Pyrazole Derivatives: An Insight." Anti-Infective Agents 18, no. 3 (2020): 207–23. http://dx.doi.org/10.2174/2211352517666191022103831.

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Background: Due to newly emerging microbial infections and the development of resistance against cutting-edge therapeutics, innovative and robust medicinal agents are required. Small ring heterocycles, such as pyrazole and its derivatives have been acknowledged to possess myriad biological properties and the presence of pyrazole in clinics like celecoxib, phenylbutazone (anti-inflammatory), CDPPB (antipsychotic), rimonabant (anti-obesity), antipyrine, difenamizole (analgesic), fipronil (broad-spectrum insecticidal), betazole (H2-receptor agonist) and fezolamide (antidepressant) drugs has prove

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Urbonavičius, Arminas, Sonata Krikštolaitytė, Aurimas Bieliauskas, et al. "Synthesis and Characterization of New Pyrano[2,3-c]pyrazole Derivatives as 3-Hydroxyflavone Analogues." Molecules 28, no. 18 (2023): 6599. http://dx.doi.org/10.3390/molecules28186599.

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In this paper, an efficient synthetic route from pyrazole-chalcones to novel 6-aryl-5-hydroxy-2-phenylpyrano[2,3-c]pyrazol-4(2H)-ones as 3-hydroxyflavone analogues is described. The methylation of 5-hydroxy-2,6-phenylpyrano[2,3-c]pyrazol-4(2H)-one with methyl iodide in the presence of a base yielded a compound containing a 5-methoxy group, while the analogous reaction of 5-hydroxy-2-phenyl-6-(pyridin-4-yl)pyrano[2,3-c]pyrazol-4(2H)-one led to the zwitterionic 6-(N-methylpyridinium)pyrano[2,3-c]pyrazol derivative. The treatment of 5-hydroxy-2,6-phenylpyrano[2,3-c]pyrazol-4(2H)-one with triflic

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M. Mohareb, Rafat, Maher H.E. Helal, Amany E. Mayhoub, and Amira E.M. Abdallah. "Multi-component reactions for the synthesis of pyrazolo [1,5-a]quinoline derivatives together with their cytotoxic evaluations." Bulletin of the Chemical Society of Ethiopia 37, no. 3 (2023): 717–34. http://dx.doi.org/10.4314/bcse.v37i3.14.

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ABSTRACT. A new approaches for the synthesis of novel pyrazolo[1,5-a]quinazoline 8a-f and pyrazolo[1,5-a]quinazolin-6-one 10a-s and 12a-s derivatives were obtained using 4-(2-phenylhydrazono)-4H-pyrazol-3-amine derivatives 5a-f via their multi-component reactions. The later pyrazole derivatives were prepared via arylhydrazone derivatives 3a-f. The structures of the synthesized compounds were established based on their respective analytical data. On the other hand, the cytotoxic effects of the synthesized compounds were obtained against the six cancer cell lines, namely A549, HT-29, MKN-45, U87

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Bertolasi, Valerio, Paola Gilli, Valeria Ferretti, Gastone Gilli, and Cristina Fernàndez-Castaño. "Self-assembly of NH-pyrazoles via intermolecular N—H...N hydrogen bonds." Acta Crystallographica Section B Structural Science 55, no. 6 (1999): 985–93. http://dx.doi.org/10.1107/s0108768199004966.

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The crystal structures of two NH-pyrazole derivatives forming intermolecular N—H...N hydrogen bonds are reported: 5-methyl-4-(3-methylpyrazol-5-yl)pyrazol-3-ol, C8H10N4O (P1), and 3-methyl-5-dihydro-1H-naphtho[1,2-d]pyrazole hemihydrochloride, C12H12N2.-C12H13N_{2}^{+}.Cl− (P2). 26 other structures are surveyed in order to obtain a deeper insight into the ways NH-pyrazoles self-assemble by means of intermolecular N—H...N hydrogen bonds in molecular crystals. A limited number of compounds form chains or dimers via homonuclear N+—H...N positive-charge-assisted hydrogen bonds, typical of proton s

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Lynda, Golea. "Synthesis, DFT, Molecular docking Analysis and Antibacterial, Antioxidant Activities of tri-substituted pyrazoles." ASM Science Journal 16 (July 15, 2021): 1–7. http://dx.doi.org/10.32802/asmscj.2021.696.

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Pyrazole and its derivatives are contemplated crucial compounds in heterocyclic chemistry which are also used extensively in organic synthesis. These cycles are known for their biological and pharmacological activities. The present investigation is in the interest of some synthesized derivatives containing the pyrazole moieties. (5-Hydroxy-3,5-dimethyl-4,5-dihydro-pyrazol-1-yl)-pyridin-4-yl-methanone (1) and Furan-2-yl-(5-hydroxy-3,5-dimethyl-4,5-dihydro-pyrazol-1-yl)-methanone (2) were synthesized by cyclocondensation of the 1,3-dicarbonyl with the hydrazine derivative with a simple and rapid

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Aonofriesei, Florin. "Polysorbate 21 Can Modulate the Antibacterial Potential of Two Pyrazol Derivatives." Biomolecules 12, no. 12 (2022): 1819. http://dx.doi.org/10.3390/biom12121819.

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The combination of two compounds with known antimicrobial activity may, in some cases, be an effective way to limit the resistance to antibiotics of specific pathogens. Molecules carrying pyrazole moiety are well known for their bioactive properties and have wide applicability in the medical and pharmaceutical field. Surfactants have, among other useful properties, the ability to affect the growth of microorganisms. The paper reports on the effect of the combination of two pyrazole derivatives, (1H-pyrazol-1-yl) methanol 1-hydroxymethylpyrazole (SAM1) and 1,1′methandiylbis (1H–pyrazol) (AM1),

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40

Muhammad, Zeinab A., Fatimah Alshehrei, Mohie E. M. Zayed, Thoraya A. Farghaly, and Magda A. Abdallah. "Synthesis of Novel Bis-pyrazole Derivatives as Antimicrobial Agents." Mini-Reviews in Medicinal Chemistry 19, no. 15 (2019): 1276–90. http://dx.doi.org/10.2174/1389557519666190313095545.

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Background: bis-heterocycles especially those containing pyrazole moiety display much better antibacterial activity than mono heterocycles. Objective: Herein, we synthesised a series of new bis-pyrazoles and investigated their antimicrobial agents. Methods: A novel series of bis-pyrazole derivatives have been synthesized in good yield by coupling reaction of cyanoacetic acid 4-[(2-cyano-acetyl)-hydrazonomethyl]-benzylidene-hydrazide with a number of diazonium salts of aromatic amines in DMF in the presence of NaOH. Refluxing of the produced hydrazones with hydrazine-hydrate in ethanolic soluti

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Sawengngen, Nattawut, Petrakis N. Chalikidi, Sara Araby, Frank Hampel, Peter Gmeiner, and Olga V. Serdyuk. "Synthesis of pyrazolylvinyl ketones from furan derivatives." Organic & Biomolecular Chemistry 17, no. 19 (2019): 4850–55. http://dx.doi.org/10.1039/c9ob00701f.

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Lina A. Yaseen and Hanoy K. Al-Amood. "Preparation, Characterization, and Study of Antibacterial some new Pyrazole Derivatives." Journal of Kufa for Chemical Sciences 2, no. 9 (2023): 304–18. http://dx.doi.org/10.36329/jkcm/2022/v2.i9.13304.

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The papear include synthesis of four of pyrazole derivatives from the reaction of chalcones with substituted hydrazine. FT-IR, Mass, and H1-NMR spectra identified the compounds. The new pyrazoles (Py1-Py4) studies as anti-bacterial against negative and positive gram stain. The prepared compounds gave the high and different abilities to inhibit these bacteria according to the type of the substituted group. The inhibition ratio of pyrazole substituted by the COOH group (Py1) was 28 mm, while pyrazole substituted by OH in the meta position was less able to inhibit.

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43

Sabah, Rusul Saad, Zahraa S. Al-Garawi, and Mahmoud N. Al-jibouri. "The utilities of pyrazolines encouraged synthesis of a new pyrazoline derivative via ring closure of chalcone, for optimistic neurodegenerative applications." Al-Mustansiriyah Journal of Science 33, no. 1 (2022): 21–31. http://dx.doi.org/10.23851/mjs.v33i1.1067.

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Pyrazolines and their derivatives have been extensively studied as coordinated ligands of high potential applications in diverse chemical and biological systems. This work explores some methods of synthesis of pyrazolines, such as the preparation of pyrazole derivatives via chalcones. It also demonstrates that 2-pyrazoline complexes were biologically active and have had a range of clinical applications. Palladium (II) complex of pyrazole was active as antitumor when tested against murine mammary adenocarcinoma (LM3). Copper (II) and Cobalt (II) complex are biologically active in the living sys

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Gharat, Vaishnav D., and Vishvanath D. Patil. "Multicomponent synthesis of pyrazole-3-one under mild conditions using an effective novel ceria-doped copper nanocatalyst." Research Journal of Chemistry and Environment 29, no. 1 (2024): 52–60. https://doi.org/10.25303/291rjce052060.

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Synthesis of pyrazole-3-one derivative was successfully catalyzed by a copper nanocatalyst that had been doped with cerium. With outstanding yields of pyrazol- 3-one derivatives, this approach has been applied to a wide range of substrates including electrophilic and sterically hindered aromatic aldehydes. The remarkable selectivity under mild conditions of this commercially available inexpensive catalyst is an attractive feature of this method.

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Atiya, Rana N., Zahraa L. Razzaq, Widad I. Yahya, and Helen M. Neamah. "Synthesis, Characterization and Studying Biological Activity of Heterocyclic Compounds." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 13, no. 01 (2023): 205–11. http://dx.doi.org/10.25258/ijddt.13.1.31.

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Heterocyclic moiety was mentioned to present diverse biological activities such as inhibitors of protein glycation, antibacterial, antifungal, anticancer, antidepressant, anti-inflammatory, antituberculosis, antioxidant, and as antiviral agents, in addition to other biological activities; therefore, many medicines containing heterocyclic moiety have been observed. Due to the pharmacological importance of heterocyclic derivatives, the present work comes as attempt to synthesis of heterocyclic compound involved (tetrazole and pyrazole rings) by series of steps starting from pyrimidin-2-amine, wh

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Dawood, Kamal M., Ahmad M. Farag, and Zaghloul E. Kandeel. "Heterocyclic Synthesis via Enaminonitriles: One-pot Synthesis of Some New Pyrazole, Isoxazole, Pyrimidine, Pyrazolo[1,5-a]pyrimidine, Pyrimido[1,2-a]benzimidazole and Pyrido[1,2-a]benzimidazole Derivatives." Journal of Chemical Research 23, no. 2 (1999): 88–89. http://dx.doi.org/10.1177/174751989902300211.

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Yadav, Amrita, Sushil Kumar, Navneet Dwivedi, Rajiv Gupta, and Narendra Kumar Singh. "Synthesis, Docking Studies and Anticancer Activity of Some Pyrazole Derivatives." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 34, no. 04 (2024): 453. https://doi.org/10.59467/ijhc.2024.34.453.

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A series of pyrazole derivatives (2a-m) was synthesized by the reaction of pongamol with various hydrazines (1a-m) derivatives. All the synthesized pyrazoles (2a-m) were screened for their anticancer potential against breast carcinoma (MCF7, MDA-MB-231), ovarian carcinoma (SKOV3) HeLa cervical cancer cells, and HEK293 and MCF10A normal cells. Among 13 compounds, seven compounds PONG, 2j, 2k, 2e, 2m, 2h, and 2g were found to have more than 50% cell inhibition. Docking study of synthesized compounds was also performed for enzyme CYP1A1 using SWISS DOCK.. KEYWORDS :CYP1A1, Doxorubicin, MTT, Ponga

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Cetin, Adnan, and Havva Kurt. "Synthesis, Antibacterial Activity and Molecular Docking Studies of New Pyrazole Derivatives." Letters in Drug Design & Discovery 17, no. 6 (2020): 745–56. http://dx.doi.org/10.2174/1570180816666190905155510.

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Background: The pyrazole structure is an important heterocyclic structure and plays critical roles in agriculture, industrial and medicine. Furthermore, compounds containing pyrazole are known to exhibit various biological properties such as antibacterial, antifungal, anticancer, antiinflammatory, antidepressant, antipyretic, antiviral, anti-tubercular and anti-HIV activities. Because of these properties, pyrazole molecules have become a very popular topic for organic chemists. Methods: A series newly substituted pyrazole molecules were synthesized and characterized. Their antimicrobial activi

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Tangeti, Venkata S., Kattaru R. Babu, Dasari Vasundhara, K. V. V. V. Satyanarayana, Himabindu Mylapalli, and Kaja S. P. Kumar. "One Pot Synthesis of Novel Substituted 2',4'-Dihydrospiro[chroman-2,3'-pyrazol]-4- one Derivatives." Current Organic Synthesis 15, no. 2 (2018): 267–74. http://dx.doi.org/10.2174/1570179414666171011161836.

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Aim and Objective: In the work, we have successfully presented a synthetic route for the synthesis of novel 2',4'-dihydrospiro[chroman-2,3'-pyrazol]-4-one derivatives via one pot multicomponent approach. Materials and Method: Substituted 2',4'-dihydrospiro[chroman-2,3'-pyrazol]-4-one were prepared through cascade three-component condensation of ortho-hydroxyacetophenone, β-ketoester, hydrazine in the presence of pyrrolidine as a catalyst under ethanol reflux conditions. Results: A series of novel 2',4'-dihydrospiro[chroman-2,3'-pyrazol]-4-one have been synthesized through a facile strategy. Th

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Vashisht, Ketan, Pooja Sethi, Anshul Bansal, et al. "Path of Pyrazoles from Synthetic Factors to Anti-inflammatory Potential: A Review." Asian Journal of Chemistry 36, no. 6 (2024): 1217–31. http://dx.doi.org/10.14233/ajchem.2024.31652.

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Pyrazoles, a class of heterocyclic compounds, have garnered considerable attention in drug development due to their intriguing properties, particularly those containing a pyrazole moiety. Pyrazole, a pivotal chemical in the creation of potent bioactive agents, encompasses five heterocyclic members. The discovery of certain pyrazole compounds exhibiting robust biological activities has spurred interest in this field of inquiry. Heterocyclic compounds incorporating nitrogen and its derivatives have historically served as crucial sources of medicinal compounds. Given that the heterocyclic group c

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