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

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Published: 3 June 2025

Last updated: 6 July 2025

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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: Chalcones were used to synthesis series of 2-pyrazoline derivatives and evaluated their antimicrobial and anti-inflammatory activities (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 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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11

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 heterocycles. The melting points of these compounds were determined using APP. Digital ST 15 melting point apparatus. SP3-100 spectrophotometer recorded FT-IR spectra (KBr) (cm-1). NMR spectra (&#948;, ppm) were recorded on 400 MHz AVANCE-III High-Performance FT-NMR Spectrometer BRUCKER (Switzerland) and some 1H NMR spectra were recorded on Varian EM-360L NMR Spectrophotometer (90 MHz) (USA) in CDCl3 or DMSO-d6 as a solvent. Elemental analyses were carried out at a Vario EL C, H, N, and S Analyzer. Bromine was determined using direct titration method after carius combustion. </P><P> Results: The structures of the compounds were confirmed by IR, 1H NMR, 13C NMR, and elemental analyses. </P><P> Conclusion: 1,3-Diphenyl-1H-pyrazole-4-carboxladehyde 1 and 2-pyrazoline derivative 9 confirmed their importance in the synthetic organic chemistry. Depending on the formyl group of aldehyde 1 and active methylene of pyrazoline 8, we synthesized new series of heterocycles; indol-2,3-dione, trizolo[3,4-a]benzazole, thiazolo[2,3-a]benzimidazole-3-one and pyrazolyl-pyrazoline derivatives expecting their pharmacological applications. The targeted compounds were substantiated from its spectral data.</p>

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Ahmed A. ALKazmi, Farouq Emam Hawais, and Yuosra K. Alasadi. "Synthesis and Characterization of some Pyrazoline derivatives from Chalcones containing azo and ether groups." Tikrit Journal of Pure Science 22, no. 9 (2023): 69–75. http://dx.doi.org/10.25130/tjps.v22i9.877.

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A number of 3-(substituted)-5-(2((4-chlorobenzyl)oxy)-5-(m-tolyldizenyl) pheny l) pyrazoline (3a-j) have been synthesized by benzyloxation of hydroxyl group to give the substrate 2-((4-chlorobenzyl)oxy)-5-(m-tolyldizenyl) benzaldehyde (1). The compound (1) has been treated with different substituted acetophenone to give a new series of chalcone derivatives 1-(substituted)-3-(2-((4-chlorobenzyl)oxy)-5-(m-tolyldiazenyl) phenyl) prop-2-en-1-one (2a-j). The chalcone derivatives have been treated with hydrazine hydrate according to Michael addition reaction to afford a series of new pyrazoline derivatives. The characterization of the newly synthesized compounds elucidated by FT-IR, 1H-NMR, 13C-NMR, 13C-DEPT and elemental analyses

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13

Journal, Baghdad Science. "Synthesis of New Heterocyclic Derivatives from 4-(3, 5-Dimethyl-1-phenyl-1H-pyrazol-4-ylazo)- benzoic acid." Baghdad Science Journal 7, no. 1 (2010): 727–36. http://dx.doi.org/10.21123/bsj.7.1.727-736.

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In this work pyrazolin derivatives were prepared from the diazonium chloride salt of 4-aminobenzoic acid. Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, acetyl acetone to obtain the corresponding hydrazono derivative (1). Cyclocondensation reaction of compounds (1) with hydrazine hydrate and phenyl hydrazine in boiling ethanol affording the corresponding pyrazoline-5-one derivatives of 4-aminobenzoic acid (2,3). Then compound (3) was reacted with thionyl chloride to give the corresponding acid chloride derivative(4), followed by conversion into the corresponding acid hydrazide derivative (5) carboxylic acid thiosemicarbazide (11), esters (14,15), thioesters (16,17) and amides (18,19), when treated hydrazine hydrate, thiosemicarbazide, alcohols, alkylthiol and secondary amines in dry refluxing benzene; respectively. Schiff's bases (6-8) were prepared by refluxing of compound (5) with different aldehydes and ketons, then two compounds from the Schiff's bases were cyclized with ?-mercapto acetic acid to give (9 and 10). Furthermore, 1,2,4-triazole derivative (12) have been also prepared by refluxing thiosemicarbazide derivative with sodium hydroxide solution (4%) followed acidification of the result using (10%)hydrolic acid. Moreover, a thiadiazole derivative (13) has been prepared by treatment of thiosemicarbazide derivative with concentrated sulfuric acid as cyclyzing agent. Finally, oxadiazole derivative (20) has prepared by condensation of its acid hydrazide derivative with carbon disulfide in basic medium.

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Özdemir, Ahmet, Belgin Sever, and Mehlika Dilek Altıntop. "New Benzodioxole-based Pyrazoline Derivatives: Synthesis and Anticandidal, In silico ADME, Molecular Docking Studies." Letters in Drug Design & Discovery 16, no. 1 (2018): 82–92. http://dx.doi.org/10.2174/1570180815666180326152726.

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Background: Azoles are commonly used in the treatment and prevention of fungal infections. They suppress fungal growth by acting on the heme group of lanosterol 14α-demethylase enzyme (CYP51), thus blocking the biosynthesis of ergosterol. </P><P> Objectives: Due to the importance of pyrazolines in the field of antifungal drug design, we aimed to design and synthesize new pyrazoline-based anticandidal agents. Methods: New pyrazoline derivatives were synthesized via the reaction of 1-(chloroacetyl)-3-(2- thienyl)-5-(1,3-benzodioxol-5-yl)-2-pyrazoline with aryl thiols. These compounds were evaluated for their in vitro antifungal effects on Candida species. Docking studies were performed to predict the affinity of the most effective anticandidal agents to substrate binding site of CYP51. Furthermore, MTT assay was performed to determine the cytotoxic effects of the compounds on NIH/3T3 mouse embryonic fibroblast cell line. A computational study for the prediction of ADME properties of all compounds was also carried out. Results: Compounds 5, 8, 10 and 12 were found as the most potent anticandidal agents against Candida albicans and Candida glabrata in this series with the same MIC values of ketoconazole and they also exhibited low toxicity against NIH/3T3 cells. Docking results indicated that all these compounds showed good binding affinity into the active site of CYP51. In particular, chloro substituted compounds 8 and 12 bind to CYP51 through direct coordination with the heme group. According to in silico studies, compound 8 only violated one parameter of Lipinski’s rule of five, making it a potential orally bioavailable agent. Conclusion: Compound 8 was defined as a promising candidate for further in vitro and in vivo studies.

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Kaur, Amandeep, Baljeet Kaur, and Monika Gupta. "SYNTHESIS AND BIOLOGICAL EVALUATION OF 1-SUBSTITUTED-2-THIENYL- 5-(4-CHLOROPHENYL) PYRAZOLINE DERIVATIVES AS ANTIPROLIFERATIVE AGENTS." INDIAN DRUGS 56, no. 06 (2019): 24–30. http://dx.doi.org/10.53879/id.56.06.11849.

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Cancer is not a single disease, but a large group of diseases characterized by uncontrolled, rapid and pathological proliferation of abnormally transformed cells. Pyrazoline is a five-membered heterocyclic ring having two adjacent nitrogen atoms within the ring. It has only one endocyclic double bond and is basic in nature. The present study involves synthesis of 1-substituted-2-thienyl-5-(4-chlorophenyl) pyrazoline derivatives. The synthesized compounds were subjected to anticancer screening against SK-OV-3 cells line to determine the growth inhibitory effects of the compounds. Amongst all the derivatives in series (6a-j), the pyrazoline derivatives exhibited potent anticancer activity. All synthesized compounds possessed good to moderate anticancer activity. Compounds 6b and 6c at concentration 80 μg/mL possessed % control growth inhibition comparable to standard drug andriamycin. The order for the % control growth inhibition of SK-OV-3 was found to be 6h> 6j> 6f> 6i> 6e> 6g> 6d> 6a. All the compounds inhibited 50 % of the cell growth at the conc.

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Abdollahi-Alibeik, Mohammad, Ali Moaddeli, and Kianoosh Masoomi. "BF3 bonded nano Fe3O4 (BF3/MNPs): an efficient magnetically recyclable catalyst for the synthesis of 1,4-dihydropyrano[2,3-c]pyrazole derivatives." RSC Advances 5, no. 91 (2015): 74932–39. http://dx.doi.org/10.1039/c5ra11343a.

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1,4-Dihydropyrano[2,3-c]pyrazole derivatives were efficiently synthesized in a simple one-pot three-component reaction of various aldehydes with malononitrile and a 2-pyrazoline-5-one in the presence of BF<sub>3</sub>/MNPs as a novel nanostructured, heterogeneous and reusable catalyst.

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Mohammed Qadir, Kale, Hawzhin Yassen Hussein, Marlin Yousef Aziz, et al. "Synthesis, molecular docking study and antibacterial activity of new pyrazoline derivatives." Bulletin of the Chemical Society of Ethiopia 39, no. 5 (2025): 955–66. https://doi.org/10.4314/bcse.v39i5.

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In this study, a new series of pyrazoline compounds with five members was synthesized by cyclization of chalcone derivatives in presence of phenyl hydrazine (3a-i). The development began with 4-hydroxy acetophenone, which was benzylated via Williamson ether synthesis to give 1-(4-(benzyloxy) phenyl)-3-phenylprop-2-en-1-one (1), many derivatives of chalcones (2a-i) were synthesized by Claisen-Schmidt condensation of the compound (1) with substituted benzaldehyde, chalcones undergo cyclization with phenyl hydrazine to give target pyrazoline derivatives. The structure of all newly obtained compounds was supported by spectral data (FT-IR, 1H-NMR, 13C-NMR and 13C DEPT-135). Some pyrazoline derivatives were estimated for their antibacterial activity against Escherichia coli as Gram-negative and Staphylococcus aureus as Gram-positive. The results showed the high sensitivity of the synthesized compounds to both types of bacteria. Furthermore, this study examines a molecular docking analysis of synthesized compounds, the results revealed a favorable binding contact with the target bacterial DNA gyrase (PDB ID: 1KZN) of E. coli. Finally, combined findings indicate that these compounds exhibit significant antibacterial activity, with computer models suggesting their ability to target bacterial enzymes or receptors, thereby inhibiting their function and suppressing bacterial growth. KEY WORDS: Chalcone, Pyrazoline, Antibacterial activity, Docking study Bull. Chem. Soc. Ethiop. 2025, 39(5), 955-966. DOI: https://dx.doi.org/10.4314/bcse.v39i5.11

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E. Hawaiz, Farouq, and Mohammad K. Samad. "Synthesis and Spectroscopic Characterization of Some New Biological Active Azo–Pyrazoline Derivatives." E-Journal of Chemistry 9, no. 3 (2012): 1613–22. http://dx.doi.org/10.1155/2012/525940.

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A number of 3-[4-(benzyloxy)-3-(2-Chlorophenylazo)-phenyl]-5-(substituted-phenyl)-1-substituted-2-pyrazolines( 4a-j) and (5a-j) have been synthesized by diazotization of 2-chloroaniline and its coupling reaction with 4-hydroxy acetophenone, followed by benzyloxation of the hydroxyl group to give the substrate [4-benzyloxy-3-(2-chlorophenylazo)-acetophenone (1)].The prepared starting material (1) has been reacted with different substituted benzaldehydes to give a new series of chalcone derivatives 1-[(4-benzyloxy)-3-(2-chloro-phenylazo)-phenyl]-3-(substituted phenyl)-2-propen-1-one (3a-j), in high yields and in a few minutes, and the later compounds were treated with hydrazine hydrate according to Michael addition reaction to afford a new biolological active target compounds (4a-j) and (5a-j). Furthermore, The structures of the newly synthesized compounds were confirmed by FT-IR,13C-NMR,13C-DEPT &1H-NMR spectral data. The chalcone and pyrazoline derivatives were evaluated for their anti bacterial activity againstEscherichia colias gram negative andStaphylococcus aureusas gram positive, the results showed significant activity against both types of bacteria.

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V., Nagaraju, Srinivasulu R., Doraswamy K., and Venkata Ramana P. "Synthesis, characterization and antibacterial screening of new pyrazole and pyrazoline-5-one derivatives." Journal of Indian Chemical Society Vol. 88, Feb 2011 (2011): 293–98. https://doi.org/10.5281/zenodo.5773547.

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Department of Chemistry, Sri Krishnadevaraya University, Anantapur-515 003, Andhra Pradesh, India Department of Chemistry, Sri Krishnadevaraya University Post-Graduate Centre, Kurnool-518 002, Andhra Pradesh, India <em>E-mail </em>: ramanapv2103@yahoo.com <em>Manuscript received 21 July 2009, revised 10 May 2010, accepted 07 July 2010</em> A series of N' -(p-toluene sulphonyl)-3-methyl-4-(substituted arylhydrazono)-2-pyrazoline-5-ones and N' -(2- hydroxybenzoyl)-3,5-dimethyl-4-(substituted arylazo)pyrazoles have been synthesized and characterized by chemical analysis, IR and <sup>1</sup>H NMR spectral data. The compounds have been screened for antibacterial activity against Staphylococcus aureus and Escherichia coli.

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Al-Ghulikah, H. A., A. S. El-Azab, M. S. AL-Saleem, M. S. AL-Towayan, and S. A. Al-Issa. "Green synthesis, characterization, biological evaluation and docking study of some pyrazoline and pyrimidine derivatives." Research Journal of Chemistry and Environment 25, no. 12 (2021): 88–97. http://dx.doi.org/10.25303/2512rjce8897.

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Green and classical techniques have been utilized for preparing of a variety of aryl - substituted pyrazoline and pyrimidine derivatives (2-8). Reactions of chalcones 1 with semicarbazide and thiosemicarbazide, nicotinic acid hydrazide and amino guanidine hydrochloride afforded the corresponding N-substituted pyrazoline derivatives 2-5. Pyrimidine derivatives 6-8 were achieved via reaction of chalcone derivatives 1 with several reagents namely: guanidine nitrate, thiourea and 6-amino-2-thioxo-2,3- dihydropyrimidin-4(1H)-one under conventional and ultrasonic conditions. Ultrasonic method was found to be an easy work-up procedure and it gave high yield in comparison with conventional method. The structures of new synthesis compounds were characterized by elemental and spectral analyses. Some of newly compounds were tested in vitro antibacterial activity against some gram–positive and gram–negative. The antimicrobial results displayed favorable antimicrobial activity. Molecular docking has been perfomed for compound 5b using MOE 2008.10, The data results obtained are quite promising.

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Shailesh, H. Shah, and S. Patel Pankaj. "Synthesis and antimicrobial activity of azetidin-2-one containing pyrazoline derivatives." Journal of Indian Chemical Society Vol. 90, Jun 2013 (2013): 863–66. https://doi.org/10.5281/zenodo.5773732.

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Department of Chemistry, Patel J.B.R. Arts, Patel A.M.R. Commerce & Patel J.D.K.D. Science College, Borsad-388 540, Gujarat, India <em>E-mail </em>: shailchem@yahoo.com Department of Chemistry, Sheth L.H. Science College, Mansa, Gujarat, India <em>Manuscript received online 25 July 2012, revised 26 July 2012, accepted 31 July 2012</em> Pyrazolines are well-known and important nitrogen containing 5-membered heterocyclic compounds and various methods have been worked out for their synthesis. A new series of 3-chloro-1-{ 4-[5-(substituted phenyl)-4,5-dihydropyrazol-3-yl]phenyl}-4-(4-cholorophenyl)azetidin-2.-one are synthesized by reacting 3-chloro-1-{ 4-[3-(substituted phenyl)prop2-enoyl]phenyl}-4-(4-chlorophenyl)azetidin-2-one with 99% hydrazine hydrate. All these compounds were characterized by means of their IR, <sup>1</sup>H NMR, spectroscopic data and microanalysis. All the synthesized products were evaluated for their antimicrobial activity. All the compounds were tested for their antibacterial and antifungal activities by broth dilution method.

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B. jadhav, S., R. A. shastri, K. V. gaikwad, and S. V. gaikwad. "Synthesis and Antimicrobial Studies of Some Novel Pyrazoline and Isoxazoline Derivatives." E-Journal of Chemistry 6, s1 (2009): S183—S188. http://dx.doi.org/10.1155/2009/361564.

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A new series of 1H-3-(4’-substituted phenyl)-5-(6’’-methoxy napthaline)-2-pyrazolines (4a-e) and 1H-3-(4’-substituted phenyl)-5-(6’’-methoxynapthaline)-2-isoxazolines (5a-e) were synthesized by reacting 1-(4’-substituted phenyl)-3-(6’’-methoxynapthaline)-2-propene-1-one (3a-e) with hydrazine hydrate and hydroxylamine hydrochloride respectively. All these compounds were characterized by means of their IR,1H NMR, spectroscopic data and microanalysis. All the synthesized products were evaluated for their antimicrobial activity. All the compounds exhibited significant to moderate antimicrobial activity.

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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 (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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Komal, Savaliya, and S. Patel Pankaj. "Synthesis and Biological evaluation Of Some New Benzoyl Pyrazole Derivatives bearing a 6,8-Dibromo-2-methylquinazolin-4-one Moiety." Der Pharma Chemica 14, no. 2 (2022): 6. https://doi.org/10.4172/0975-413X.14.2.1-5.

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A new series of 3-[4-(1-benzoyl-5-(substitutedphenyl)-4,5-dihydro-pyrazol-3-yl)phenyl]-6,8-dibromo-2-methylquinazolin-4-one have been synthesized by the condensation reaction of 6,8-dibromo-3-{4-[5-(substitutedphenyl)-4,5-dihydro-pyrazol-3-yl]phenyl}-2-methylquinazolin-4-one with benzoyl chloride by using pyridine as a solvent. The intermediate have been synthesized by refluxation of 6,8-dibromo-3-{4-[3- (substitutedphenyl)prop-2-enoyl]phenyl}-2-methylquinazolin-4-one (0.01M) and 99% hydrazine hydrate (0.015M) by using ethanol (50ml) as a solvent with various aldehydes. The chemical structures of synthesized benzoyl pyrazoline derivatives were characterized by their IR, NMR and spectral data. The newly synthesized compounds were screened for their antibacterial and antifungal activities by Agar Cup method

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Savaliya, Komal, and S. Patel Pankaj. "Synthesis and Biological evaluation Of Some New Benzoyl Pyrazole Derivatives bearing a 6,8-Dibromo-2-methylquinazolin-4-one Moiety." Der Pharma Chemica 14, no. 2 (2022): 6. https://doi.org/10.5281/zenodo.13353950.

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A new series of 3-[4-(1-benzoyl-5-(substitutedphenyl)-4,5-dihydro-pyrazol-3-yl)phenyl]-6,8-dibromo-2-methylquinazolin-4-one have been synthesized by the condensation reaction of 6,8-dibromo-3-{4-[5-(substitutedphenyl)-4,5-dihydro-pyrazol-3-yl]phenyl}-2-methylquinazolin-4-one with benzoyl chloride by using pyridine as a solvent. The intermediate have been synthesized by refluxation of 6,8-dibromo-3-{4-[3- (substitutedphenyl)prop-2-enoyl]phenyl}-2-methylquinazolin-4-one (0.01M) and 99% hydrazine hydrate (0.015M) by using ethanol (50ml) as a solvent with various aldehydes. The chemical structures of synthesized benzoyl pyrazoline derivatives were characterized by their IR, NMR and spectral data. The newly synthesized compounds were screened for their antibacterial and antifungal activities by Agar Cup method.

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26

D., N. Satyanarayana, K. Ravindranath L., Ravi Sankar T., and Venkata Ramana P. "Electrochemical behaviour of 1-benzenesulfonyl-3-benzenesulfanantido-4-(4'-substituted- arylhydrazono)-2-pyrazolin-5-ones." Journal of India Chemical Society Vol 81, Aug 2004 (2004): 654–59. https://doi.org/10.5281/zenodo.5830003.

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Department of Chemistry, Sri Krishnadevaraya University, Anantapur-515 003, India Department of Chemistry, Sri Krishnadevaraya University Post-Graduate Centre, Kurnool-518 002, India <em>E-mail</em> : ramanapeddakotla@yahoo.co.in         <em>Fax</em>: 91-8518-276183 <em>Manuscript received 4 October 2002. revised 10 December 2003. accepted 10 March 2004</em> The electrochemical behaviour of 1- benzenesulfonyl-3-benzenesulfanamido-4- (4' -substituted-arylhydrazono )-2-pyrazolin-5- ones has been investigated at dme and ge electrodes in buffer solutions of pH 1.1-10.2 using de polarography, cyclic voltammetry and coulometry. The compounds exhibit one well defined wave in acidic solutions and two waves in alkaline solutions. The process is irreversible and diffusion-controlled. Preparative controlled potential electrolysis indicates that aromatic amine and 1-benzenesulfonyl-3-benzenesulfanamido-4-amino-2-pyrazolin-5-one are products of electrolysis. The mechanism of the reduction and the effect of solvent composition have been studied.

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27

Oral, Basak. "The synthesis and antitubercular activity of substituted hydrazone,2-pyrazoline-5-one and 2-isoxazoline-5-one derivatives possessing 1,3,4-thiadiazole moiety." MARMARA PHARMACEUTCAL JOURNAL 3, no. 16 (2012): 222–28. http://dx.doi.org/10.12991/201216402.

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28

Prabha, B., C. Raja, S. Nathiya, and M. R. Ezhilarasi. "Synthesis, in vitro and in silico Studies of Naphthalene Pyrazoline Prop-2-en-1-one Derivatives." Asian Journal of Chemistry 32, no. 8 (2020): 1849–56. http://dx.doi.org/10.14233/ajchem.2020.22654.

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The synthesized new naphthalene pyrazoline prop-2-en-1-one derivatives (NDPP 1-8) were obtained by the Michael addition reaction of ethyl propanoate, hydrazine hydrate with NPD as a multicomponent scaffold. (E)-1-(naphthalen-3-yl)-3-phenylprop-2-en-1-one (NPD) was formed from 2-acetyl naphthalene and substituted aldehyde via Claisen-Schmidt condensation reaction. The NDPP skeleton structures were confirmed by infrared, 1H & 13C NMR spectral data and elemental analysis. The structure of NDPP compounds was subjected to molecular docking and ADME studies. The result of ADME prediction, compound NDPP 2, which contains electron withdrawing -Cl group has high drug-likeness value 4.21 than the compounds NDPP 4 and 7 which had electron donating CH3 and OCH3 group shows the drug-likeness value 2.62. The NDPP 2 also has high drug score 0.63 than NDPP 4 and NDPP 7 have drug score 0.60 and 0.69, respectively. Docking studies shows that compound NDPP 5 which also contain electron withdrawing NO2 group has good binding affinity value -8.8 Kcal/mol were docked with 1UAG protein. These compounds showed good drug-likeness value 2.25 and drug score 0.65. in vitro Studies have a high inhibition value for the same NO2 substituted derivative. All the compounds have higher binding affinity value than standards binding affinity value.

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29

Nagaraju, V., R. Srinivasulu, K. Doraswamy, and P. Venkata Ramana. "ChemInform Abstract: Synthesis, Characterization and Antibacterial Screening of New Pyrazole (VI) and Pyrazoline-5-one Derivatives (III)." ChemInform 43, no. 3 (2011): no. http://dx.doi.org/10.1002/chin.201203106.

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30

Güniz Küçükgüzel, Ş., Sevim Rollas, Habibe Erdeniz, Muammer Kiraz, A. Cevdet Ekinci, and Aylin Vidin. "Synthesis, characterization and pharmacological properties of some 4-arylhydrazono-2-pyrazoline-5-one derivatives obtained from heterocyclic amines." European Journal of Medicinal Chemistry 35, no. 7-8 (2000): 761–71. http://dx.doi.org/10.1016/s0223-5234(00)90179-x.

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31

Abdula, Ahmed Mutanabbi, Ghazwan Ali Salman, and Hamid H. Mohammed. "Comparative Study on Conventional and Ultrasound Irradiation Promoted Synthesis of 2,3-Disubstitutedquinoxaline Derivatives." Al-Mustansiriyah Journal of Science 28, no. 3 (2018): 141. http://dx.doi.org/10.23851/mjs.v28i3.207.

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A series of ten chalcone-substituted quinoxalines (4a-e), (3a-e) starting from 1-(phenylquinoxalin-2-yl)ethanone and 1-(3-methylquinoxalin-2-yl)ethanone have been synthesized using conventional heating and ultrasound-assisted methods. Furthermore, novel of five quinoxaline derivatives including pyrazoline, isoxazole, pyrimidin-2-one, N-acylpyrazoline and pyridin-2-one moieties were also prepared from the reaction of chalcone compound 4a with different cyclization reagents using the same strategy. The structures of all synthesized compounds were established on the basis of FT-IR, 1H-NMR and 13C-NMR. The ultrasonic irradiation method provide several advantages over conventional heating method, including shorter reaction times (30-90 min.) and good percentage yields (65% - 88%), comparing with conventional protocol (5 to 20 hrs. with 30% to 55% reaction yields).

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32

Maurya, Ram C., and Deen D. Mishra. "Synthesis and physico-chemical studies of some novel mixed-ligand cyanonitrosyl {CrNO}5 complexes of chromium with 2-3-pyrazoline-5-one derivatives." Transition Metal Chemistry 12, no. 6 (1987): 551–52. http://dx.doi.org/10.1007/bf01023847.

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33

Kuecuekguezel, S. Gueniz, Sevim Rollas, Habibe Erdeniz, Muammer Kiraz, A. Cevdet Ekinci, and Aylin Vidin. "ChemInform Abstract: Synthesis, Characterization and Pharmacological Properties of Some 4-Arylhydrazono-2-pyrazoline-5-one Derivatives Obtained from Heterocyclic Amines." ChemInform 31, no. 45 (2000): no. http://dx.doi.org/10.1002/chin.200045136.

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34

Maurya, R. C., R. Verma, and D. Sutradhar. "Synthesis, Magnetic, and Spectral Studies of Mixed‐Ligand Complexes of Nickel(II) Involving Some Chelating 4‐Oximino‐2‐pyrazoline‐5‐one Derivatives." Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry 33, no. 3 (2003): 435–51. http://dx.doi.org/10.1081/sim-120019997.

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Maurya, R. C., D. O. Mishra, P. K. Trivedi, S. Mukherjee, and D. K. Shrivastara. "Synthesis and Characterization of Some Hovel Pehta-Coordihated Mixed-Ligakd Derivatives of Zinc(II)-bis(Acetylacetone) and-bis(Acetoacetanilide) Chelates with 2/3-Pyrazoline-5-One Derivatives." Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry 22, no. 4 (1992): 403–14. http://dx.doi.org/10.1080/15533179208020474.

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Maurya, R. C., D. D. Mishra, P. K. Trivedi, and A. Gupta. "Synthesis, Magnetic and Spectral Studies of Some Mixed-Ligand Chelates of Mercury(II) with Acetoacetanilide/o-hydroxyacetophenone and 2/3-Pyrazoline-5-one Derivatives." Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry 24, no. 1 (1994): 17–28. http://dx.doi.org/10.1080/00945719408000091.

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37

Maurya, R. C., R. Verma, P. K. Trivedi, and H. Singh. "Synthesis, Magnetic and Spectral Studies of Some Mixed-Ligand Chelates of Bis(2-Hydroxyacetphenonauam)Copper(II) with 2- or 3-Pyrazoline-5-One Derivatives." Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry 28, no. 2 (1998): 311–29. http://dx.doi.org/10.1080/00945719809351906.

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38

Maurya, R. C., D. D. Mishra, S. Mukherjee, P. K. Trivedi, and S. K. Jaiswal. "Synthesis and Structural Investigation of Some Mixed-Ligand Cyanonitrosyl {Mo(NO)2}6Complexes of Molybdenum with some 2 or 3-Pyrazoline-5-one Derivatives." Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry 23, no. 5 (1993): 723–34. http://dx.doi.org/10.1080/15533179308016855.

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Maurya, R. C., D. D. Mishra, and V. Filial. "Synthesis and Characterization of Some Mixed-Ligand Thiocyanato Complexes of Cadmium(II), Mercury(II), Zinc(II) with 2-or 3-Pyrazoline-5-One Derivatives." Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry 25, no. 1 (1995): 139–50. http://dx.doi.org/10.1080/15533179508218209.

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40

Maurya, R. C., D. D. Mishra, R. Rathore, and S. Jain. "Synthesis, Magnetic and Spectral Studies of Some Mixed-Ligand Complexes of Copper(II) and Cobalt(II) with Schiff Bases and 2- or 3-Pyrazoline-5-one Derivatives." Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry 24, no. 3 (1994): 427–39. http://dx.doi.org/10.1080/00945719408000122.

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41

Maurya, R. C., J. Chourasia, M. H. Martin, S. Roy, A. K. Sharma, and P. Vishwakarma. "Dioxomolybdenum(VI) chelates of bioinorganic, catalytic, and medicinal relevance: Studies on some cis-dioxomolybdenum(VI) complexes involving O, N-donor 4-oximino-2-pyrazoline-5-one derivatives." Arabian Journal of Chemistry 8, no. 3 (2015): 293–306. http://dx.doi.org/10.1016/j.arabjc.2011.01.010.

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42

Maurya, R. C., J. Dubey, and B. Shukla. "A Sincle-Step and Virtually Single Pot Synthesis of some Cynonitrosyl {Mn(NO)2}7Complexes of Manese(O) Involving 2/3-Pyrazoline-5-One Derivatives Directly from Manganate(VII), and Their Characterization." Synthesis and Reactivity in Inorganic and Metal-Organic Chemistry 28, no. 7 (1998): 1159–71. http://dx.doi.org/10.1080/00945719809349396.

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43

Gil-Ordóñez, Marta, Camille Aubry, Cristopher Niño, Alicia Maestro, and José M. Andrés. "Squaramide-Catalyzed Asymmetric Mannich Reaction between 1,3-Dicarbonyl Compounds and Pyrazolinone Ketimines: A Pathway to Enantioenriched 4-Pyrazolyl- and 4-Isoxazolyl-4-aminopyrazolone Derivatives." Molecules 27, no. 20 (2022): 6983. http://dx.doi.org/10.3390/molecules27206983.

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A series of N-Boc ketimines derived from pyrazolin-5-ones have been used as electrophiles in enantioselective Mannich reactions with different 1,3-dicarbonyl compounds. This method provides a direct pathway to access the 4-amino-5-pyrazolone derivatives bearing a quaternary substituted stereocenter and containing two privileged structure motifs, the β-diketone and pyrazolinone substructures. The adducts were obtained in excellent yields (up to 90%) and enantioselectivities (up to 94:6 er) by employing a very low loading of 2 mol% of a quinine-derived bifunctional squaramide as an organocatalyst for a wide range of substrates. In addition, the utility of the obtained products was demonstrated through one step transformations to enantioenriched diheterocyclic systems (4-pyrazolyl-pyrazolone and 4-isoxazolyl-pyrazolone), potentially promising candidates for drug discovery.

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44

A. Avery, Mitchell, Jae-Chul Jung, and E. Blake Watkins. "Synthesis and Cyclization Reaction of Pyrazolin-5-one Derivatives." HETEROCYCLES 65, no. 1 (2005): 77. http://dx.doi.org/10.3987/com-04-10216.

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45

Jung, Jae C., E. Blake Watkins, and Mitchell A. Avery. "EFFICIENT SYNTHESIS OF 4-ETHOXYCARBONYL PYRAZOLIN-5-ONE DERIVATIVES." Synthetic Communications 32, no. 24 (2002): 3767–77. http://dx.doi.org/10.1081/scc-120015395.

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46

Liu, Man, Chen-Fei Liu, Jing Zhang, Yan-Jun Xu, and Lin Dong. "Correction: Metal-free tandem reaction synthesis of spiro-cyclopropyl fused pyrazolin-5-one derivatives." Organic Chemistry Frontiers 6, no. 7 (2019): 1064–65. http://dx.doi.org/10.1039/c9qo90021g.

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47

Chauhan, Pankaj, Suruchi Mahajan, and Dieter Enders. "Asymmetric synthesis of pyrazoles and pyrazolones employing the reactivity of pyrazolin-5-one derivatives." Chemical Communications 51, no. 65 (2015): 12890–907. http://dx.doi.org/10.1039/c5cc04930j.

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The various catalytic asymmetric strategies employing organo- and metal-catalysts utilized pyrazolin-5-one derivatives for the synthesis of potentially bioactive enantiopure pyrazoles and pyrazolones are presented.

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48

RAJEEV, JAIN, and K. PARDASANI H. "Synthesis of some New Pyrazole and Pyrazolin-5-one Derivatives of Sulphonamides." Journal of Indian Chemical Society Vol. 68, Jul 1991 (1991): 415–16. https://doi.org/10.5281/zenodo.6158217.

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School of Studies in Chemistry, Jiwaji University, Gwalior-474 011 <em>Manuscript received 17 January 1991, revised 17 June 1991, accepted 26 June 1991</em> Synthesis of some New Pyrazole and Pyrazolin-5-one Derivatives of Sulphonamides.

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Yagi, Kazuo, Akira Numata, Norihiko Mimori, Toshiro Miyake, Kazutaka Arai, and Shigeru Ishii. "Synthesis and insecticidal activity of novel 1,3,4-oxadiazolin-5-one and pyrazolin-5-one derivatives." Pesticide Science 55, no. 2 (1999): 161–65. http://dx.doi.org/10.1002/(sici)1096-9063(199902)55:2<161::aid-ps881>3.0.co;2-m.

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50

C., P. SINGH. "Synthesis of N1-(2-Pyridinecarbony 1)-3-methyl-4(substituted-hydrazono)-2-pyrazolin-5-one." Journal of Indian Chemical Society Vol. 62, Mar 1985 (1985): 222–23. https://doi.org/10.5281/zenodo.6322071.

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Chemical Laboratories, Sahu Jain College, Najibabad-248 763 <em>Manuscript received 27 </em>April <em>1981, accepted 25 February 1985</em> 2-Pyridinecarboxylic acid hydrazide and their derivatives are generally used as antibacterial agent. N<sup>1</sup>-(2-Pyridinecarbonyl)-3-methyl-4-substituted hydrazono)-2-pyrazolin-5-one and their derivatives have been synthesised. Their Rf values, chemical analysis, it and nmr spectra are recorded.

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