Academic literature on the topic 'Pyrazoline-5- one derivatives'

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Journal articles on the topic "Pyrazoline-5- one derivatives"

1

N., Hariraj1* N. Kannappan2 Siju.E.N3. "Synthesis of certain Pyrazoline 5-One Derivatives of 6-Methyl Nicotinicacid and Evaluation of their Antimicrobial activities." Journal of Pharma Research 1, no. 2 (2012): 16–17. https://doi.org/10.5281/zenodo.1098657.

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<strong><em>ABSTRACT</em></strong> <em>Pyrazolines are known to possess a wide variety of biological activities. Due to the wide range of biological activities that Pyrazolines posses, it was our aim to prepare pyrazolin-5-one derivatives containing substituted Nicotinic acid and to explore, their therapeutic advantage. Among the six newly synthesized pyrazoline-5-one derivatives MPZ-1 showed promising antimicrobial activity even at a concentration 250mcg/disc. and MPZ-2 showed moderate antimicrobial activity at a concentration 500mcg/disc.</em> <strong><em>Keywords: </em></strong><em>Pyrazoline-5- one derivatives, substituted Nicotinic acid, Antibacterial, antifungal.</em>
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2

Gineinah, Magdy. "6-, 7- AND 8-(5-ARY L-1-PHENYL-2-PYRAZOLIN-3-LY)IMIDAZO- AND PYRIMIDO[2,1-b]BENZOTHIAZOLES AS NOVEL ANTICONVULSANT AGENTS." Scientia Pharmaceutica 69, no. 1 (2001): 53–61. http://dx.doi.org/10.3797/scipharm.aut-01-06.

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Some new derivatives of 2-amino-5- and 6-(5-aryl-1-phenyl-2-pyrazolin-3-yl)benzothiazole were synthesized from the corresponding aminophenyl compounds by reaction with KSCN/Br2 to build up the benzothiazole ring. The aminophenyl derivatives of pyrazoline were prepared by cyclization with phenylhydrazine of the appropriate 1,3-diphenyl-2-propen-1-one derivatives obtained from arninoacetophenone and differently substituted aldehydes. However, the newly synthesized 2-aminobenzothiazole derivatives of pyrazoline were subjected to cyclization with ethyl brornopyruvate to afford the formation of 6- and 7-(5-aryl-1 -phenyl-2-pyrazolin-3 -yl)-2-ethoxycarbonylimidazo[2,1-b]benzothiazole derivatives. Furthermore, dimethyl acetylenedicarboxylate (DMAD) was used as another cyclizing agent for 2-aminobenzothiazole derivatives to obtain 7- and 8-(5-aryl-1-phenyl-2-pyrazolin-3-y1)-4-methoxycarbonyl-2-oxo-2H-pyrimido[2,1-b]benzothiazole derivatives. The newly prepared compounds were screened for their anticonwlsant activities. However, some of the tested compounds manifested good anticonvulsant potencies.
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3

Fatmayanti, Baiq Risma, Ahmad Habibie, and Anselmania Kartini Dhey. "SYNTHESIS OF CHALCONE AND PYRAZOLINE DERIVATIVES WITH ACETOPHENONE AND VERATRALDEHYDE AS PRECURSORS." Medical Sains : Jurnal Ilmiah Kefarmasian 9, no. 3 (2024): 655–64. http://dx.doi.org/10.37874/ms.v9i3.1274.

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Chalcones and pyrazolines are heterocyclic compounds with promising biological and pharmaceutical activities. Chalcone and pyrazoline can be found in different sources, such as natural and synthetic compounds. This study aimed to explore the synthesis of chalcone and pyrazoline derivatives with acetophenone and veratraldehyde as precursors. Chalcone was successfully synthesized through the Claissen-Schmidt reaction between acetophenone and veratraldehyde at room temperature 25-30 ºC and mediated by KOH as a base catalyst for 20 hours. The corresponding substituted pyrazoline derivative was also successfully synthesized through a cyclocondensation reaction between the synthesized chalcone and phenylhydrazine as starting materials under reflux conditions at temperatures of 75-80 ºC for 4 hours. The Chalcone A derivative compound obtained was (E)-3-(3,4-dimethoxy phenyl)-1-phenyl prop-2-en-1-one (Chalcone A). The Pyrazoline A derivative compound was obtained as pyrazole compound 5-(3,4-dimethoxy phenyl)-1,3-diphenyl-4,5-dihydro-1H-pyrazole (pyrazoline A). Chalcone A and Pyrazoline A obtained as yellowish and brownish-orange powders in 14.89 % and 66.57 % yields, respectively. The chastities of Chalcone A and Pyrazoline A was 98.55 % and 88.54 %, respectively. A qualitative identification for both synthesized compounds was performed using normal-phase thin-layer chromatography which revealed the Rf value for Chalcone A and Pyrazoline A was 0.43 (in mobile phase ethyl acetate:n-hexane 3:1 v/v) and 0.55 (in mobile phase DCM:n-hexane 3:1 v/v), respectively. Moreover, the elucidation structure of synthesized compounds using FTIR and GC-MS instruments revealed the structure of synthesized Chalcone A and Pyrazoline A agrees with the theoretical structure of Chalcone A and Pyrazoline A. Keywords: Synthesis, Chalcone, Pyrazoline, Acetophenone, Veratraldehyde
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4

Mistry, Rakesh N., and K. R. Desai. "Studies on Synthesis of Some Novel Heterocyclic Chalcone, Pyrazoline, Pyrimidine - 2 - One, Pyrimidine - 2 - Thione,para-Acetanilide Sulphonyl and Benzoyl Derivatives and their Antimicrobial Activity." E-Journal of Chemistry 2, no. 1 (2005): 30–41. http://dx.doi.org/10.1155/2005/953107.

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1, 2 - Dichloro benzene on chlorosulphonation by chlorosulphonic acid gives 1, 2 - [dichloro] - benzene sulphonyl chloride which on condensation withp–amino acetophenone gives 1-[acetyl] - 1’ , 2’ - [dichloro] - dibenz sulphonamide derivative. This derivative undergo condensation with 2,4- dichloro benzaldehyde gives 1- [3” - (sub. phenyl) - 2” - propene - 1” - one] - 1’ , 2’ - [dichloro] - dibenz sulphonamide derivative which on reaction with 99% hydrazine hydrate and glacial acetic acid gives 1-[acetyl]-3- [1’ , 2’ - (dichloro) - dibenz sulphonamide] -5 - [2” , 4” - dichloro phenyl] - 2 - pyrazoline derivative. This derivative reacts with various substituted aldehydes to give corresponding substituted chalcone derivatives [1(a-j)]. Now, these chalcone derivatives [1(a-j)] on condensation with urea gives corresponding substituted pyrimidine - 2 - one derivatives [2(a-j)] and on condensation with thio-urea gives corresponding substituted pyrimidine- 2 -thione derivatives [3(a-j)]. Further, these chalcone derivatives [1(a-j)] on reaction with 99% hydrazine hydrate gives 1 - [1’ - (H) - 5’ - (sub. phenyl) - 2’ - pyrazoline]- 3 - [1” , 2” - (dichloro) - dibenz sulphonamide] - 5 - [2’’’ , 4’’’ - dichloro phenyl]-2- pyrazoline derivatives [4(a-j)] as an intermediate compounds, which on condensation with p-acetanilide sulphonyl chloride gives corresponding substituted p - acetanilide sulphonyl derivatives [5(a-j)] and on condensation with benzoyl chloride gives corresponding substituted benzoyl derivatives [6(a-j)]. Structure elucidation of synthesised compounds has been made on the basis of elemental analysis, I.R. spectral studies and 1H N.M.R. spectral studies. The antimicrobial activity of the synthesised compounds has been studied against the cultures “Staphylococcus aureus”, “Escherichia coli” and “Candela albicans”.
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5

Al-Smaisim, Rafah F., Redha E. Al-Bayati, and Abdul Hussain K. Sharba. "Synthesis of New Heterocyclic compounds derived from Pyrazoline-5-one compound." Al Mustansiriyah Journal of Pharmaceutical Sciences 9, no. 1 (2011): 123–31. http://dx.doi.org/10.32947/ajps.v9i1.278.

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In this work new heterocyclic pyrazolin derivatives have been synthesized from diazonium chloride salt of 4-aminobenzoic acid: firstly, Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, (ethyl acetoacetate)obtain the corresponding hydrazono derivative (1). Secondly, Cyclocondensation reaction of compound (1) with hydrazine hydrate (2) in boiling ethanol affording the corresponding pyrazoline-5-one. Then compound (2) reacted with thionyl chloride to give the corresponding acid chloride derivative(3), followed by conversion into the corresponding carboxylic acid thiosemicarbazide (4), esters (7-9), thioesters (10), (11), and amides (12-14), when treated hydrazine hydrate, thiosemicarbazide, alcohols, alkylthiol and secondary amines in dry refluxing benzene; respectively. Furthermore, 1,2,4- triazole heterocyclic ring, which might result in biologically active agents, have been prepared by refluxing thiosemicarbazide derivative (4) with sodium hydroxide solution (4%) followed acidification of the result using (10%)HCl solution. Moreover, 1, 3, 4, - thiadiazole heterocyclic ring (6) has been prepared by treatment of thiosemicarbazide derivative with concentrated sulfuric acid as cyclization agent. Finally, derivative (15) has prepared by reflux (1) with phydroxybenzaldehydethen the product reflux with 5-amino-1, 3, 4-thiadiazol-2- thiol to product (16) derivative. All structures of newly synthesized compounds have been characterized and identified via of their physical properties and spectral data analysis (IR, UV.)
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6

Mervat Mohammed K and Tagreed N-A Omar. "Synthesis, Characterization, Anti-Inflammatory, and Antimicrobial Evaluation of New 2-Pyrazolines Derivatives Derived from Guaiacol." Iraqi Journal of Pharmaceutical Sciences( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) 32, Suppl. (2023): 254–61. http://dx.doi.org/10.31351/vol32isssuppl.pp254-261.

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Abstract:&#x0D; Chalcones were used to synthesis series of 2-pyrazoline derivatives and evaluated their antimicrobial and anti-inflammatory activities&#x0D; (E)-1,3-diphenylprop-2-en-1-one (1-5) were synthesized by Claisen-Schmidt Condensation method through the reaction of acetophenone with five various para substituted benzaldehyde in presence of KOH, the reaction monitoring by TLC and the result intermediates were checked by melting point and FT-IR&#x0D; Various 2-Pyrazoline derivatives were prepared by one pot reaction that involved the refluxing of (E)-1,3-diphenylprop-2-en-1-one (1–5) and Hydrazine monohydrate in the presence of glacial acetic acid for 24 hours at a temperature of (45–50) °C for a duration 24 hrs. pyrazoline II (1-5) was formed, then antioxidant compound (guaiacol) was added reflex for 24-48 hours, monitoring by TLC to ensure the reaction was completed. The final mixture was cooled in ice-water bathe until the formation of crystals were completed, added to crushed ice, kept in refrigerator overnight, filter, recrystallized and then dried to get 2-pyrazoline derivatives, IIIa, IIIb, IIIc, IIId and, IIIe. based on the spectral data 2-pyrazoline derivatives structures have been confirmed. The synthesized compounds were screened for their antimicrobial activity and anti-inflammatory.
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7

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 system as biomolecules or co factors. Based on these information, we tried here to synthesis a new 2-pyrazoline from (E)-3-(4-bromophenyl)-1-(pyridin-2-yl)prop-2-en-1-one. The newly synthesized pyrazoline was characterized using mass spectroscopy, nucleic magnetic resonance spectroscopy NMR and Fourier transform infrared spectroscopy FTIR. The characterization results showed that 2-pyrazoline has successfully synthesized. The microanalyses (C.H.N.S), GC-MS, H and 13C NMR and FT-IR spectra confirmed the formation of 2-pyrazoline ring with substitution at N1,C-3 and C-5 and the spin-spin coupling constants (J) for the multiple peaks at H NMR spectra pointed to the de shielded aromatic protons in α and β protons of the prepared chalcone. Interestingly, some new family of pyrazoles that have isosteres of Zonisamide have previously showed activity toward treating neuroglial disorders such as epilepsy and autism. Thus, our synthesized pyrazole could have the potency to moderate some neurodegenerative disorders. It could negatively interact with some neurotransmitters through hydrogen bonding and electrostatic interactions with the amino and carboxylic ends of the functional ends of the neurotransmitters. This promising trend by the promising candidate 2- pyrazoline should have further investigations.
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8

El-Ossaily, Y. A. B., R. M. Zaki, and S. A. Metwally. "Investigation and Synthesis of Some Novel Spiro Heterocycles Related to Indoline Moiety." Journal of Scientific Research 6, no. 2 (2014): 293–307. http://dx.doi.org/10.3329/jsr.v6i2.17590.

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Reactions of indole-2,3-dione 1 with 2-mercaptobenzimidazole, o-phenylenediamine, 2-aminophenol, 2-aminobenzothiazole, 2-aminobenzimidazole and 3-methyl-1-phenyl-2-pyrazolin-5-one were carried out to give compounds spiroindolethiazetobenzimidazole 2, spirobenzimidazole(oxazole)indoline 3a,b, benzothiazol(imidazol) iminoindolinone 4a,b and methyloxoindolylidenepyrazolone 5 respectively. Compound 5 was reacted with 2-aminophenol as well as o-phenylenediamine to give new spirooxazepine and diazepine derivatives 6a,b respectively. Reaction of 5 with nitrogen nucleophiles as well as carbon nucleophiles was investigated to furnish new spiro heterocycles 7-11. The reaction of 2-(2-oxo-1,2-dihydroindol-3-ylidene)malononitrile compound 12 with 3-methyl-1-phenyl-2-pyrazoline-5-one was carried out to give spiroindolopyranopyrazolo derivative 13. Compounds 4a,b was reacted with thioglycolic acid to give thiazolidinone derivatives 14a,b. Epoxidation of 5 using monoperoxyphthalic acid magnesium salt hexahydrate and hydrogen peroxide were executed to afford the novel dispiro (2-pyrazolin oxiraneindoline)dione compound 15. The chemical structures of the synthesized compounds were well established by elemental and spectral analyses. Keywords: Spiroheterocycles; Epoxidation; Diazapines, Oxazepines; Spirothiazolidinone. © 2014 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved. doi: http://dx.doi.org/10.3329/jsr.v6i2.17590 J. Sci. Res. 6 (2), 303-317 (2014)
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9

Yuosra K. Alasadi, Farouq Emam Hawais, and Ahmed A. ALKazmi. "Synthesis and Characterization of Some New Pyrazoline Derivatives Containing Azo Group by One Pot Method." Tikrit Journal of Pure Science 23, no. 3 (2018): 67–74. http://dx.doi.org/10.25130/tjps.v23i3.502.

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This research includes the preparation of some of pyrazoline derivatives containing the azo group by one pot method through the treatment of the compound 2-hydroxy-5-(m-tolyldiazenyl) benzaldehyde with p-chlorob enzylchloride to give the compound(1) using the Williamson reaction. The compound (1) is treated with a series of ketones and with phenylhydrazine in the base medium to give new derivatives of pyrazoline (2-11). The synthesized compounds were characterized by elemental analyses and FT-IR, 1H-NMR, 13C-NMR, 13C-DEPT.
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10

Rathinamanivannan, S., K. Megha, Raja Chinnamanayakar, Ashok Kumar, and M. R. Ezhilarasi. "Synthesis and Characterization of 2-Pyrazoline Derivatives and their in silico and in vitro Studies on Antimicrobial and Anticancer Activities." Asian Journal of Chemistry 31, no. 10 (2019): 2191–96. http://dx.doi.org/10.14233/ajchem.2019.22082.

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The new series of 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives were synthesized by cyclization method using biphenyl chalcone with n-butyric acid and hydrazine hydrate. The synthesized 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives chemical structures were confirmed from spectral data such as FT-IR, 1H and 13C NMR. 2-Pyrazoline derivatives were docked with bacterial (1UAG) and breast cancer (1OQA) protein. Based on high binding affinity score, the best compound was subjected to in vitro anticancer activity by MTT assay. Also, antimicrobial activity were studied for synthesized 2-pyrazoline derivatives.
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