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Relevant bibliographies by topics / 5-dihydro-1H-pyrazoles

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Academic literature on the topic '5-dihydro-1H-pyrazoles'

Author: Grafiati

Published: 4 June 2021

Last updated: 11 February 2022

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Journal articles on the topic "5-dihydro-1H-pyrazoles"

1

Chovatia, P. T., J. D. Akabari, P. K. Kachhadia, P. D. Zalavadia, and H. S. Joshi. "Synthesis and selective antitubercular and antimicrobial inhibitory activity of 1-acetyl-3,5-diphenyl-4,5-dihydro-(1h)-pyrazole derivatives." Journal of the Serbian Chemical Society 71, no. 7 (2006): 713–20. http://dx.doi.org/10.2298/jsc0607713c.

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The new compounds 1-aryl-3-{1-phenyl-3-[p (methylthio)phenyl]pyrazol-4-yl}-2-propen-1-ones 2a?l were prepared by the condensation of 1-phenyl-3-[p (methylthio)phenyl]-4-formylpyrazole 1 with different aryl ketones. Compounds 2a?l in reaction with hydrazine hydrate yielded 3-aryl-5-{1-phenyl-3-[p-(methylthio)phenyl]pyrazol-4 yl}-4,5-dihydro-(1H)-pyrazoles 3a?l and in the presence of hydrazine hydrate in glacial acetic acid gave 1-acetyl-3-aryl 5-{1-phenyl-3-[p-(methylthio)phenyl]pyrazol-4-yl}-4,5 dihydro-(1H)-pyrazoles 4a?l. These compounds were tested in vitro for their antitubercular and antimicrobial activities. The in vitro antimycobacterial activity of the newly synthesized compounds was investigated against Mycobacterium tuberculosis H37RV (ATCC 27294) in BACTEC 12B medium using the ALAMAR radiometric system. The antimicrobial in vitro activity was tested against Bacillus coccous, Bacillus subtilis Escherichia coli, Proteus vulgaris and antifungal activity against Aspergillus niger. The structures of the synthesized compounds were assigned on the basis of elemental analysis IR, 1H NMR and mass spectral data.

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2

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 chemical shifts (δ, ppm) of Ha, Hb, Hc, CH3 protons, C=N, C=O and CH3 carbons of 1-(3-(3,4-dichlorophenyl)-5-(substitutedphenyl)-4,5-dihydro-1H-pyrazole-1-yl) ethanones have been assigned and correlated with Hammett substituent constants and Swain-Lupton’s parameters using single and multi-regression analysis. From the results of statistical analyses the effect of substituents on the above group frequencies and chemical shifts of the acetylated pyrazoles were discussed.

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3

Altıntop, Mehlika Dilek. "Synthesis, In vitro and In silico Evaluation of a Series of Pyrazolines as New Anticholinesterase Agents." Letters in Drug Design & Discovery 17, no. 5 (May 18, 2020): 574–84. http://dx.doi.org/10.2174/1570180816666190618111023.

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Background: Pyrazolines, electron-rich nitrogen carriers, are of great importance due to their potential applications for the treatment of many diseases including inflammation, infectious diseases and neurodegenerative disorders. Objectives: The purpose of this work was to synthesize new pyrazoline derivatives and evaluate their anticholinesterase effects. Methods: 1-Aryl-5-[4-(piperidin-1-yl)phenyl]-3-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazoles (1-7) were synthesized via the treatment of 1-(3,4-dimethoxyphenyl)-3-[4-(piperidin-1-yl)phenyl]prop-2- en-1-one with arylhydrazine hydrochloride derivatives in acetic acid, whereas 1-aryl-5-[4- (morpholin-4-yl)phenyl]-3-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazoles (8-14) were obtained by the treatment of 1-(3,4-dimethoxyphenyl)-3-[4-(morpholin-4-yl)phenyl]prop-2-en-1-one with arylhydrazine hydrochloride derivatives in acetic acid. Their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were determined using a modification of Ellman’s spectrophotometric method. In silico docking and Absorption, Distribution, Metabolism and Excretion (ADME) studies were performed using Schrödinger’s Maestro molecular modeling package. Results: In general, piperidine derivatives were found to be more effective than morpholine derivatives on cholinesterases (ChEs). 1-Phenyl-5-[4-(piperidin-1-yl)phenyl]-3-(3,4-dimethoxyphenyl)- 4,5-dihydro-1H-pyrazole (1) and 1-(4-cyanophenyl)-5-[4-(piperidin-1-yl)phenyl]-3-(3,4- dimethoxyphenyl)-4,5-dihydro-1H-pyrazole (7) were identified as the most effective AChE inhibitors in this series with 40.92% and 38.98%, respectively. Compounds 1 and 7 were docked into the active site of human AChE (PDB code: 4EY7). Both the compounds were found to be capable of forming π-π stacking interactions with Trp286. Based on in silico ADME studies, these compounds are expected to have reasonable oral bioavailability. Conclusion: In the view of this work, the structural modification of the identified agents is going on for the generation of new anticholinesterase agents with enhanced efficacy.

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4

Dorn, Helmut, and R�diger Ozegowski. "LINK Synthesis with 3-Hydroxy-1H-pyrazoles: 3-Carboxyisoalkyloxy-1H-pyrazoles - bicyclic acylpyrazolium salts and ?-Lactams - 3-Carboxyisoalkyloxy-4,5-dihydro-1H-pyrazol-5-ones." Journal f�r Praktische Chemie/Chemiker-Zeitung 340, no. 5 (1998): 437–49. http://dx.doi.org/10.1002/prac.19983400506.

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5

Pasin, J. S. M., A. P. O. Ferreira, A. L. L. Saraiva, V. Ratzlaff, R. Andrighetto, P. Machado, S. Marchesan, et al. "Antipyretic and antioxidant activities of 5-trifluoromethyl-4,5-dihydro-1H-pyrazoles in rats." Brazilian Journal of Medical and Biological Research 43, no. 12 (December 2010): 1193–202. http://dx.doi.org/10.1590/s0100-879x2010007500139.

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6

Odin, I. S., A. A. Golovanov, V. V. Bekin, and V. S. Pisareva. "Synthesis and Acylation of 3-Aryl-5-(2-phenylethynyl)-4,5-dihydro-1H-pyrazoles." Chemistry of Heterocyclic Compounds 49, no. 11 (January 25, 2014): 1687–90. http://dx.doi.org/10.1007/s10593-014-1421-7.

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7

Burde, P. C., and A. M. Rahatgaonkar. "Facile Synthesis and Biological Evaluation of Cyclopropyl-Pyrazole Hybrids in [bmim][PF6]-Water Biphasic System as Antifungal Agents." Asian Journal of Organic & Medicinal Chemistry 4, no. 3 (September 30, 2019): 152–58. http://dx.doi.org/10.14233/ajomc.2019.ajomc-p192.

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3-Cyclopropyl-5-(4-substituted)-1-phenyl-4,5-dihydro-1H-pyrazoles derived from corresponding chalcones were synthesized and evaluated for their biological activities. A convenient synthesis of a library of these compounds in 1-butyl-3-methylimidazolium hexafluorophosphate-water biphasic system at ambient temperature has been accomplished. The ionic liquid, [bmim][PF6] and water which are immiscible, has been easily recycled and reused after separation of the products without any noticeable diminution in its activity.

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8

Venkata Narsimha Reddy, Chintalapani, Eligeti Rajanarendar, and Ananthula Krishnamurthy. "Synthesis of 3-methyl-1,5-diphenyl-7-aryl-7,8-dihydro-6H-pyrazolo[4,5-b]azepines." Collection of Czechoslovak Chemical Communications 55, no. 4 (1990): 1055–58. http://dx.doi.org/10.1135/cccc19901055.

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3,5-Dimethyl-4-nitro-1-phenylpyrazole (I) on treatment with chalcones II under phase transfer conditions gives the Michael adducts, 3-methyl-4-nitro-1-phenyl-5-(2-aryl-4-phenyl-4-oxo-1-butyl)pyrazoles (III). The Michale adducts on cycloreduction with stannous chloride-hydrochloric acid furnish 3-methyl-1,5-diphenyl-7-aryl-7,8-dihydro-6H-pyrazolo[4,5-b]azepines (IV). IR, 1H NMR, 13C NMR and mass spectra support the structures of III and IV.

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9

Agre, Neha, Mihir Khambete, Arundhati Maitra, Antima Gupta, Tulika Munshi, Sanjib Bhakta, and Mariam Degani. "Exploration of 5‐(5‐nitrothiophen‐2‐yl)‐4,5‐dihydro‐1H‐pyrazoles as selective, multitargeted antimycobacterial agents." Chemical Biology & Drug Design 95, no. 1 (October 14, 2019): 192–99. http://dx.doi.org/10.1111/cbdd.13624.

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10

Sviridova, L. A., A. N. Tavtorkin, N. A. Shalynina, N. I. Vorozhtsov, P. S. Protopopova, Zh S. Urmambetova, and K. A. Kochetkov. "Synthesis of 4,5-dihydro-1H-pyrazoles with chiral substituents at position 3 or 5." Russian Chemical Bulletin 64, no. 5 (May 2015): 1078–82. http://dx.doi.org/10.1007/s11172-015-0981-8.

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