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Journal articles on the topic 'Acetophenone derivative'

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Published: 5 June 2025

Last updated: 15 July 2025

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Kantlehner, Willi, Jochen Mezger, Hansjörg Lehmann, Kai Edelmann, and Wolfgang Frey. "Orthoamide und Iminiumsalze, XCVa. Umsetzungen von Orthoamiden von Alkin-Carbonsäuren mit Acetophenonen und Acetophenon-Phenylhydrazonen." Zeitschrift für Naturforschung B 73, no. 10 (2018): 689–701. http://dx.doi.org/10.1515/znb-2018-0065.

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AbstractThe orthoamides of alkyne carboxylic acids 4 react with acetophenones 5 – catalyzed by trialkylborates – to give ketene aminals 6, which can be transformed to 5-amino-5-hydrazino-penta-2,4-dien-1-ones 10 by treatment with 2,4-dinitro-phenylhydrazine. From acetophenone-phenylhydrazones 12 and orthoamides 4 1H-1,2-diazepines 18 (fett) are formed at room temperature, whereas 4-dimethylamino-pyridines 22 are obtained at elevated temperatures. The diazepine 18a is degraded to the pyridine-derivative 22b upon heating. The N-unsubstituted acetophenone-hydrazone 25 reacts with 4c to give amidrazone 26. The constitution of compounds 18a, 22a, 22b, 26 is established by crystal structure analyses.

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Hammouda, M., A. S. El-Ahl, Y. M. El-Toukhee, and M. A. Metwally. "Reactions of Ketonic Mannich Bases with Malononitrile and Malononitrile dimer." Journal of Chemical Research 2002, no. 2 (2002): 89–94. http://dx.doi.org/10.3184/030823402103171258.

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The reaction of malononitrile with the tertiary Mannich base hydrochloride derived from acetophenone and some related compounds 1, 3, 5 and 7, in piperidine at 50°C afforded the pyrido[1,2-a]pyrimidine derivatives 2, tetrahydronaphthalene derivative 4 substituted quinolines 6 and benzopyran derivatives 8. While the condensation of malononitrile dimer with acetophenone, cyclohexanone and/ or α-tetralone Mannich bases hydrochloride 1, 3 and 9 gave the pyridine, isoquinoline and benzo[f]isoquinoline derivatives 10–12 in moderate to good yield.

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Patel, Pineshkumar N., and Denish C. Karia. "Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif." International Letters of Chemistry, Physics and Astronomy 69 (August 2016): 42–48. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.69.42.

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Novel series of diversely substituted acetyl pyrazoline having biphenyl carbonitrile motif have been synthesized. The reaction of 2-cyno-4’-bromomethyl biphenyl with1-(4-hydroxy-phenyl)-ethanone resulted in acetophenone derivative of biphenyl-2-carbonitrile. This acetophenone derivative was condensed with substituted aromatic aldehyde in mixed solvent resulted in various substituted chalcones. These chalcones were further cyclized using hydrazine hydrate in presence of glacial acetic acid to produce titled compound derivatives. The chemical structures of synthesized compounds were elucidated by 1H-NMR, 13C-NMR FT-IR and mass spectra. Synthesized compounds were screened for their antimicrobial activity by broth dilution method. Out of twelve newly synthesized compounds, eight compounds are found to be equipotent to Ampicillin.

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Patel, Pineshkumar N., and Denish C. Karia. "Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif." International Letters of Chemistry, Physics and Astronomy 69 (August 12, 2016): 42–48. http://dx.doi.org/10.56431/p-al2z39.

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Sudhanshu, Saxena, та C. Jain D. "A new acetophenone derivative from Artemisiα mαritimα". Journal of Indian Chemical Society Vol. 79, Dec 2002 (2002): 970–71. https://doi.org/10.5281/zenodo.5848477.

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Medicinal Plant Chemistry Division, Central Institute of Medicinal and Aromatic Plants, Lucknow-226 015. India E-mail : root@cimap.sirnet.ernet.in     Fax : 91-0522-342676 Manuscript received 21 December 2001, revised 4 April 2002. accepted 16 July 2002 A new acetophenone derivative 2-hydroxy-4,6-dimethoxyaeetophenone (1) along with a-santonin and 5-hydroxy-7.4'-dimethoxy-flavonc have been isolated from the aerial parts of Artemisiα mαritimα.

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Qi, Xiao Yan, Lin Wu, Jian Guo Wang, and De Lian Yi. "A Novel Synthesis of Acetophenone Benzopyran Derivative." Advanced Materials Research 152-153 (October 2010): 1483–86. http://dx.doi.org/10.4028/www.scientific.net/amr.152-153.1483.

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The development of a novel synthesis of acetophenone benzopyran is reported. A acetophenone benzopyran derivative was prepared from 1-(2,4-dihydroxyphenyl)ethanone (3) through O-prenylation and Lewis acids catalyzed intermolecular cyclization reaction. The structure of product 1-(3,4-dihydro-4,4-dimethyl-7-hydroxy-2H-1- benzopyran -6-yl)- ethanone (1) was characterized by UV, IR, 1H-NMR, 13C-NMR and elemental analysis.

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Giap, Tran Huu, Ha Thi Thoa, Vu Thi Kim Oanh, et al. "New Acetophenone and Cardanol Derivatives From Knema pachycarpa." Natural Product Communications 14, no. 6 (2019): 1934578X1985004. http://dx.doi.org/10.1177/1934578x19850046.

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Two new acetophenone derivatives named knepachycarpanone A (1) and knepachycarpanone B (2) together with a new cardanol derivative named knepachycarpanol C (3) were isolated from the EtOAc extract of Knema pachycarpa stems. Their chemical structures were established on the basis of spectral evidences. Compounds 1 and 2 exhibited moderate cytotoxicity against Hela cancer cell line with IC50 values of 26.92 ± 1.46 and 30.20 ± 1.97 μM, respectively.

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Garg, Ajay Kumar, Ranjan Kumar Singh, Vaibhav Saxena, Saurabh Kr Sinha, and Sanjay Rao. "Synthesis, Characterization, and Anti-inflammatory activity of Some Novel Oxazole Derivatives." Journal of Drug Delivery and Therapeutics 13, no. 1 (2023): 26–28. http://dx.doi.org/10.22270/jddt.v13i1.5719.

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A series of novel oxazole derivatives (A, A1, A2) were synthesized starting from acetone and urea. The compound (A) was obtained by heating it with acetophenone and urea in iodine. Compound (A) on treatment with 4-amino benzaldehyde (Z)-N-(4-amino benzylidine)-4-((E)-Penta-2, 4-diene-2) oxazole-2-amine afforded (A1). Acylation of compound (A) with 4-amino benzoyl chloride to obtain the corresponding N-(4 phenyl oxazole-2- yl)- benzamide (A2). The structures of compounds have been established employing FTIR and 1H-NMR spectral analysis. All oxazole derivatives were evaluated for anti-inflammatory activity by the carrageenan-induced Rat hind paw method. Derivative A1 shows maximum anti-inflammatory activity. Keywords: Oxazoles, anti-inflammatory, Benzamide, acetophenone, indomethacin.

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Mardjan, Muhammad Idham Darussalam, Retno Ambarwati, Sabirin Matsjeh, Tutik Dwi Wahyuningsih, and Winarto Haryadi. "SYNTHESIS OF FLAVANONE-6-CARBOXYLIC ACID DERIVATIVES FROM SALICYLIC ACID DERIVATIVE." Indonesian Journal of Chemistry 12, no. 1 (2012): 70–76. http://dx.doi.org/10.22146/ijc.21374.

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Synthesis of flavanone-6-carboxylic acid derivatives had been conducted via the route of chalcone. The synthesis was carried out from salicylic acid derivative, i.e. 4-hydroxybenzoic acid, via esterification, Fries rearrangement, Claisen-Schmidt condensation and 1,4-nucleophilic addition reactions. Structure elucidation of products was performed using FT-IR, 1H-NMR, GC-MS and UV-Vis spectrometers. Reaction of 4-hydroxybenzoic acid with methanol catalyzed with sulfuric acid produced methyl 4-hydroxybenzoate in 87% yield. The acid-catalyzed-acetylation of the product using acetic anhydride gave methyl 4-acetoxybenzoate in 75% yield. Furthermore, solvent-free Fries rearrangement of methyl 4-acetoxybenzoate in the presence of AlCl3 produced 3-acetyl-4-hydroxybenzoic acid as the acetophenone derivatives in 67% yield. Then, Claisen-Schmidt condensation of the acetophenone and benzaldehyde derivatives of p-anisaldehyde and veratraldehyde in basic condition gave 2'-hydroxychalcone-5'-carboxylic acid derivatives in 81 and 71 % yield, respectively. Finally, the ring closure reaction of the chalcone yielded the corresponding flavanone-6-carboxylic acids in 67 and 59% yield, respectively.

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Canudas, Nieves, Manuel Moreno, Sara Pekerar, Carlos Gámez, Estefania Sucre, and José E. Villamizar. "New Z-chalcones obtained from aloe-emodin: Synthesis, characterization and photophysical properties." Journal of Chemical Research 43, no. 3-4 (2019): 101–6. http://dx.doi.org/10.1177/1747519819841822.

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Three new Z-chalcone derivatives were synthesized under stereoselective conditions by condensation between an aldehyde derivative (prepared from aloe-emodin) and an acetophenone, using potassium hydroxide in dimethyl sulfoxide/H2O at room temperature. The Z configuration of the chalcone derivatives was established by nuclear magnetic resonance (NMR) studies. Photophysical properties related to the UV-Vis absorption/emission spectra and molar extinction coefficients (ε) in different solvents were determined.

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Khalifa, Nagy M., Ahmed M. Naglah, Mohamed A. Al-Omara, and Abd El-Galil E. Amr. "Synthesis and Reactions of New Chiral Linear Dipeptide Candidates Using Nalidixic Acid as Starting Material." Zeitschrift für Naturforschung B 69, no. 6 (2014): 728–36. http://dx.doi.org/10.5560/znb.2014-4031.

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A series of dipeptide heterocyclic derivatives 4-15 were synthesized using methyl 2-{[(1-ethyl- 7-methyl-4-oxo-1,4-dihydro-1,8-naphthyridin-3-yl)carbonyl]amino}-3-ethylbutanoate (3) as starting material. Treatment of 3 with L-phenylalanine methyl ester hydrochloride afforded the corresponding dipeptide methyl ester derivative 4, which was treated with hydrazine hydrate to afford the dipeptide acid hydrazide 5. Compound 5 was coupled with aldehyde and acetophenone derivatives to afford the corresponding Schiff bases 6a-f. The hydrazide derivative 5 was reacted with ethyl acetoacetate or acetone to give compounds 7 and 8, respectively. Reaction of 5 with carbon disulfide at different conditions afforded compounds 9 and 10, which were treated with hydrazine hydrate to give the 1-amino-2-dipeptido-1,3,4-triazole derivative 11. In addition, 5 was reacted with phenyl isothiocyanate to give the thiosemicarbazide derivative 12, which was cyclized with sodium hydroxide to the dipeptido 1-phenyl-1,3,4-triazole derivative 13. Finally, treatment of 13 with methyl iodide afforded the S-methyl derivative 14, which was reacted with hydrazine hydrate to give the hydrazine derivative 15.

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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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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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Marwa A. Atiyah, Olfat A. Nief, and Abdulkader M. Noori. "New Pyrazolines with Imine Moiety: Synthesis, Characterization." Tikrit Journal of Pure Science 26, no. 5 (2021): 40–47. http://dx.doi.org/10.25130/tjps.v26i5.175.

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Chalcone was prepared by claisen- schmidt condensation between reaction equivalent moles from 4-amino acetophenone with thiophen -2-carboxaldehyde in presence sodium hydroxide as base, the mechanism was involved the abstraction α Proton by base from the α-carbon of the ketone to form carbanion, which attacks carbonyl of aldehyde contains no α-hydrogens to produce α-β-unsaturated ketone, Chalcone derivative used to synthesize pyrazoline derivatives by condensation with 2,4-dinitro phenyl hydrazine. The newly synthesized compounds were determined using spectroscopic methods such as FTIR, Mass spectra, 1H-NMR.

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Ali Bawa, Ramadan, and Mona Mohammed Friwan. "Synthesis of Some Acetophenone Oximes and Their Corresponding Bridged Terphthaloyl Oxime Esters." Academic Journal of Life Sciences, no. 511 (November 2, 2019): 87–92. http://dx.doi.org/10.32861/ajls.511.87.92.

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The objective of this study is to synthesize a number of oximes along with their terphthaloyl oxime esters derived from acetophenone, 4-methylacetophenone, 4-hydroxyacetophenone, 4-aminoacetophenone and 4-nitroacetophenone as a part of ongoing research. Five acetophenone oximes have been synthesized by refluxing the acetophenone derivative with a solution of hydroxylamine hydrochloride in the presence of potassium hydroxide. The corresponding acetophenone oximes were obtained as solid materials in moderate to good yields. The structures of the resulting oximes were confirmed using IR, NMR and mass spectrometer. The HNMR data revealed that one oxime of the synthesized oximes was obtained as a mixture of two E/Z isomers in a ratio of (8:1). These resulting oximes were subjected into an esterification process with the terphthaloyl chloride in molar ratio of (1:2) respectively. The esterification reaction was carried out under basic conditions at 0 – 5 ºC then room temperature. The five corresponding bridged terphthaloyl oxime esters have been formed as solid materials in moderate yields. The structures of the obtained terphthaloyl esters were also confirmed by spectroscopic techniques such as IR, NMR and mass spec.

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Abdel-Mogib, M., S. Basaif, and T. Sobahi. "Stilbenes and a New Acetophenone Derivative from Scirpus holoschoenus." Molecules 6, no. 8 (2001): 663–67. http://dx.doi.org/10.3390/60800663.

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Lu, Yong-Fu, Si-Xuan Liu, Chun-Lin Guo, et al. "A new acetophenone derivative from Rhododendron irroratum subsp. pogonostylum." Phytochemistry Letters 61 (June 2024): 275–79. http://dx.doi.org/10.1016/j.phytol.2024.05.005.

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Lamnaouer, Driss, Fatiha Ben Khalti, Marie-Therese Martin, and Bernard Bodo. "A farnesyl acetophenone derivative from Ferula communis var. Genuina." Phytochemistry 36, no. 4 (1994): 1079–80. http://dx.doi.org/10.1016/s0031-9422(00)90496-5.

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Neamah, Rawaa, та Shaimaa Adnan. "Study the Biological Activity for Shiff Base and Β – Lactam Compounds that Synthesis and Identification from Pyrimidine Derivatives". International Journal of Pharmaceutical Quality Assurance 11, № 01 (2013): 37–39. http://dx.doi.org/10.25258/ijpqa.11.1.12.

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In This study We are synthesis and characterization of some Schiff base and β- lactam derivatives) by three steps. The First react 2-amino-4-Chloro-6-methyl pyrimidine with 4-amino acetophenone in an acid medium to get shiff base derivative(E)-4-(1-((4-Chloro-6-methyl pyridine-2-yl)imino)ethyl)aniline (1), the second step (1) react with (3,4- dimethoxybenzal dehyde,4-methyl benzaldehyde,4-dimethylamino benzaldehyde,4-bromo benzaldehyde,4–hydroxy benzaldehyde, 4-Nitro benzaldehyde) to get Schiff base derivatives (2-7), the last step (2-7) derivatives react with Chloro acetyl chloride to get –β-lactam derivatives.(8-13) All these compounds are characterization by (FTIR), (1 H-NMR),(13C- NMR). After that study, the biological activity for all these derivatives to word two kinds of bacteria study the Enzymatic and Cancer Cell.

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El-Ablack, Fawzia Zakaria. "Synthesis of Some New Benzimidazole Derivatives of Pharmaceutical Interest." E-Journal of Chemistry 8, no. 2 (2011): 748–52. http://dx.doi.org/10.1155/2011/723421.

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Reaction of 2-(aminomethyl)benzimidazole dihydrochloride (1) with ethyl acetoacetate was studied to give diazepinone-benzimidazole derivative (2), while, treatment of 1 with phenylhydrazono ethylacetoacetate afforded phenylhydrazino diazepinone derivative (3). On the other hand, reaction of 1 with acetyl acetone resulted in the formation of diazepine derivative (4). The reaction of 1 with ethyl cyanoacetate was studied to give 3-aminodiazepinone derivative (5). Also the reaction of 1 with acetophenone and/or benzophenone has been investigated to give the fused imidazolines 6 and 7 respectively, while the reaction of 1 with cyclopentanone gave benzimidazolyl derivative (8). Treatment of 1 with chloroacetyl chloride gave the fused pyrazinone (9). The treatment of 1 with benzoin gave the derivative (10). The structures of the hitherto unknown compounds have been confirmed from analytical and spectral data. The newly synthesized compounds were screened for antibacterial and antifungal activity.

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Fraga, Braulio M., Carmen E. Díaz, María Bailén та Azucena González-Coloma. "Sesquiterpene Lactones from Artemisia absinthium. Biotransformation and Rearrangement of the Insect Antifeedant 3α-hydroxypelenolide". Plants 10, № 5 (2021): 891. http://dx.doi.org/10.3390/plants10050891.

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Three new compounds, the sesquiterpenes absilactone and hansonlactone and the acetophenone derivative ajenjol, have been isolated from a cultivated variety of Artemisia absinthium. In addition, the major lactone isolated, 3α-hydroxypelenolide, was biotransformed by the fungus Mucor plumbeus affording the corresponding 1β, 10α-epoxide. A cadinane derivative was formed by an acid rearrangement produced in the culture medium, but not by the enzymatic system of the fungus. Furthermore, 3α-hydroxypelenolide showed strong antifeedant effects against Leptinotarsa decemlineata and cytotoxic activity to Sf9 insect cells, while the biotransformed compounds showed antifeedant postingestive effects against Spodoptera littoralis.

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Khalifa, Nagy M., Ahmed M. Naglah, Mohamed A. Al-Omar, Mohamed H. Abo-Ghalia, and Abd El-Galil E. Amr. "Synthesis and Reactions of New Chiral Linear Carboxamides with an Incorporated Peptide Linkage Using Nalidixic Acid and Amino Acids as Starting Materials." Zeitschrift für Naturforschung B 69, no. 3 (2014): 351–61. http://dx.doi.org/10.5560/znb.2014-3282.

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4bA series of chiral linear carboxamide derivatives (2- 15) with an incorporated peptide linkage have been prepared via the coupling of 1-ethyl-1,4-dihydro-7-methyl-4-oxo-quinoline-3-carboxylic acid (nalidixic acid, 1) with appropriate amino acid methyl esters. Coupling of 1 with amino acid methyl esters gave the corresponding peptide methyl esters 2, which were hydrolyzed with methanolic sodium hydroxide to the corresponding acids 3. Hydrazinolysis of esters 2with hydrazine hydrate afforded the corresponding acid hydrazide derivatives 4. The latter compounds were coupled with appropriate aldehydes or acetophenone derivatives to afford the corresponding Schiff base derivatives 5 and 6, respectively. The hydrazide derivative was reacted with phenyl isothiocyanate or carbonyl derivatives to give the corresponding thiosemicarbazide 7 and compounds 8- 10, respectively. Also, 4b was treated with acid monoanhydrides to give the corresponding imide derivatives 11- 13. Finally, 4b was reacted with tetracarboxylic acid dianhydride derivatives to afford the corresponding diimido carboxamide derivatives 14 and 15

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Zor, Erhan, Ahmet Saf, and Haluk Bingol. "Spectrophotometric and voltammetric characterization of a novel selective electroactive chemosensor for Mg2+." Open Chemistry 11, no. 4 (2013): 554–60. http://dx.doi.org/10.2478/s11532-012-0192-1.

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AbstractA novel azocalix[4]arene derivative, 5,11,17,23-tetrakis[(acetophenone)azo]-25,26,27,28-tetrahydroxycalix[4]arene (APC4), containing acetophenone azo groups at the upper rim was synthesized as a chemosensor. Its binding and sensing properties with alkali and alkaline earth metal ions (Li+, Na+, K+, Rb+, Cs+, Mg2+, Ca2+, Sr2+, Ba2+) were investigated by UV-vis spectrophotometric and voltammetric techniques. The stoichiometric ratio and the association constant were determined spectrophotometrically as 1:1 and (1.94±0.31)×105 L mol−1 for the complex between Mg2+ and the chemosensor, respectively. Moreover, it was shown that the interaction between Mg2+ and the APC4 occurred by means of the phenol groups at the lower rim by voltammetric methods. The results of spectrophotometric and voltammetric experiments showed that the chromogenic chemosensor has high selectivity towards Mg2+ among the other used metal ions, especially the interfering Ca2+ ion.

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Ameen, Ban, ASMAA Jawad, and Evon Akram. "Synthesis, In Vitro Biological Activity and Anti-Breast Cancer of Diazepine Derivatives." Al-Kufa University Journal for Biology 16, no. 3 (2024): 88–94. https://doi.org/10.36320/ajb/v16.i3.17437.

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Since their discovery, diazepines have been essential derivatives that can be found in nature or synthesized in laboratories. We synthesized a new diazepine (4-6), namely 2-[4-(4-chlorophenyl)-2,5-dihydro-1H-1,5-benzodiazepin-2-yl]phenol (4), 2-(4-{2-[(dioxo-l6-sulfanyl)oxy]phenyl}-2,5-dihydro-1H-1,5-benzodiazepin-2-yl)phenol (5), and 2-[4-(2-hydroxyphenyl)-4,5-dihydro-1H-1,5-benzodiazepin-2-yl]benzene-1,3-diol (6). These derivatives are synthesized from 2-hydroxy acetophenone with aldehyde derivatives, such as 4-chlorobenzaldehyde, 2-sulfobenzaldehyde, and 2,6-dihydroxybenzaldehyde. The chalcone compounds reacted with 2,4-diaminobenzene to form their final derivatives (4–6). Characterization of these derivatives by FTIR and 1H-NMR The diffusion method determines how these derivatives interact with various bacteria, such as Bacillus subtilis, S. aureus, and E. coli. The sulphonyl group in derivative 5 increase biological activity more other derivatives 4 and 6. The van der waals (vdw radius) for each atom were 1.20, 1.52, 1.70, and 11.80 for H, O, C and S atoms that calculate by used pymol.

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Mahmoud, Ahmed A., Ahmed A. Ahmed, Munekazu Iinuma, and Toshiyuki Tanaka. "Further monoterpene 5-methylcoumarins and an acetophenone derivative from Ethulia conyzoides." Phytochemistry 48, no. 3 (1998): 543–46. http://dx.doi.org/10.1016/s0031-9422(97)00907-2.

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Ishkov, Yurij V., Zinaida I. Zhilina, and Ludmila P. Barday. "The interaction of formylporphyrins with weak CH-acids." Journal of Porphyrins and Phthalocyanines 07, no. 11 (2003): 761–65. http://dx.doi.org/10.1142/s1088424603000938.

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A series of 2(α,β-unsaturated-γ-keto)-5,10,15,20-tetraphenylporphyrins was obtained by condensation of 2-formyl-5,10,15,20-tetraphenylporphyrin with acetone, 1,4-diacetylbenzene, 2-acetylthiophene, acetylacetone and acetophenone according to the Claisen-Schmidt reaction. The condensation product with 1,4-diacetylbenzene could react similarly with another formyl derivative – quinoxalin-6-carboxaldehyde and 2-formyl-5,10,15,20-tetraphenylporphyrin. It is shown that this reaction passes through formation of iminium salt formylporphyrin in presence of free base piperidine and perchloric acid.

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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, which in turn reacted with each of ethyl cyanoacetate, malononitrile, hydrazine hydrate, and thiosemicarbazide to afford the corresponding pyridine and pyrazole derivatives 13, 14, 17, and 20. The structure of newly synthesized compounds was characterized by analytical and spectroscopic data (IR, MS and NMR). All new compounds were evaluated against 5α-reductase and aromatase inhibitors and the results showed that many of these compounds inhibit 5α-reductase and aromatase activity; compound 13 was found to be the highest potency among the tested samples comparing with the reference drugs.

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Nguyen, Cong Tien, Ha Manh Bui, and Duyen Hoang My Nguyen. "Synthesis of 2-(2-(4-Phenyl-2,3-Dihydrobenzo[B][1,4]Thiazepin-2-YL) Phenoxy)-N-(P-Tolyl)Acetamide." Acta Chemica Iasi 26, no. 1 (2018): 13–20. http://dx.doi.org/10.2478/achi-2018-0002.

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Abstract The A new benzothiazepine’s derivative names N-(p-tolyl)-2-(2-(4-phenyl-2,3-dihydrobenzo[b][1,4]thiazepin-2-yl)phenoxy)acetamide was synthesized by reaction of o-aminothiophenol and N-(p-tolyl)-2-(2-(3-oxo-3-phenylprop-1-en-1-yl)phenoxy)acetamide, which was prepared from salicylaldehyde and acetophenone through (E)-3-(2-hydroxyphenyl)-1-phenylprop-2-en-1-one. The structures of the compounds were determined by IR, 1H-NMR, 13C-NMR and HR-MS spectral data.

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Lai, Peng Xiang, Qing Lin Ma, and Kyung Ho Row. "A new acetophenone derivative and other constituents from Senecio vulgaris." Journal of Chemical Research 34, no. 9 (2010): 514–16. http://dx.doi.org/10.3184/030823410x12830855365409.

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Lai, Peng Xiang, Qing Lin Ma, and Kyung Ho Row. "ChemInform Abstract: A New Acetophenone Derivative and Other Constituents from Senecio vulgaris." ChemInform 42, no. 5 (2011): no. http://dx.doi.org/10.1002/chin.201105204.

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AKTAŞ KAMİLOĞLU, Ayşe, Şahin DİREKEL, and Gonca ÇELİK. "In Vitro Leishmanicidal Activity of Different Chalcone, Phthalonitrile and Their Peripheral Tetra Zinc Phthalocyanine Derivatives." Erzincan Üniversitesi Fen Bilimleri Enstitüsü Dergisi 15, no. 3 (2022): 802–18. http://dx.doi.org/10.18185/erzifbed.1150203.

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In this study, in vitro leishmanicidal activity of different chalcone compounds (5-8), phthalonitrile derivatives (5a-8a), and zinc phthalocyanine (5b-8b) complexes bearing chalcone compound in peripheral positions were investigated. Phthalonitrile derivatives were obtained in the reaction of 4-nitrophthalonitrile with chalcone compound obtained by the reaction of acetophenone and various aldehydes. Zinc phthalocyanine complexes containing chalcone in the peripheral position were obtained as a result of the reaction of the synthesized phthalonitrile derivative with Zn(CH₃COO)₂ metal salt. The characterization of the synthesized original compounds (8, 8a and 8b) was performed by various spectroscopic methods (IR, 1H and 13C NMR, MALDI-TOF-MS and UV-Vis). Leishmaniasis is a disease lead to by parasites of the genus Leishmania, which can result in death as well as various clinical syndromes, generally in developing countries. New drug studies are needed because the drugs used in the treatment are toxic and resistance develops against them. In this study, the leishmaniacidal activities of synthesized chalcone, phthalonitrile and phthalocyanine series substances against Leishmania infantum and Leishmania major parasites were evaluated for the first time.

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Zainab Hassan Rahim and Nadia Sadiq Majeed. "Synthesis and Characterization of some new heterocyclic derivatives from terphthaldehyde and study of their biological activity." Journal of Kufa for Chemical Sciences 3, no. 1 (2023): 223–39. http://dx.doi.org/10.36329/jkcm/2023/v3.i1.12260.

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In this study, some new heterocyclic compounds have been synthesized including the preparation of some chalcone from the reaction terphthadehyde with two moles of ketone derivative p-hydroxy acetophenone in a basic medium, After that . The stage includes the preparation of new heterocyclic compounds five-membered ( pyrazole, Isoxazole) and six-membered ( oxazine, thiazine). The prepared compounds were characterized by FT-IR,1H-NMR, and 13C-NMR techniqes, in addition to their melting points and TLC (Thin Layer Chromatography).Finally,the prepared compounds are tested against Gram-positive and Gram-negative bacteria to study their biological activity.

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Rigano, Daniela, Carmen Formisano, Ester Pagano, et al. "A new acetophenone derivative from flowers of Helichrysum italicum (Roth) Don ssp. italicum." Fitoterapia 99 (December 2014): 198–203. http://dx.doi.org/10.1016/j.fitote.2014.09.019.

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Ramadan, Gomaa R. M., Eman M. Mosallam, and Thomas W. Phillips. "Methyl benzoate and its derivative, acetophenone, as fumigants to control stored product insects." Journal of Stored Products Research 105 (February 2024): 102248. http://dx.doi.org/10.1016/j.jspr.2024.102248.

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Neetu, Kumari, Khandelwal Poonam та C. Joshi Y. "Synthesis and biological activity of some novel β-diketones containing pyrazole moiety". Journal of Indian Chemical Society Vol. 91, Aug 2014 (2014): 1577–82. https://doi.org/10.5281/zenodo.5728995.

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Department of Chemistry, Mohanlal Sukhadia University, Udaipur-313 001, Rajasthan, India Department of Chemistry, University of Rajasthan, Jaipur-302 004, Rajasthan, India E-mail : drycj_16@yahoo.com Manuscript received 25 January 2014, accepted 10 February 2014 Reaction of substituted pyrazole-1-acetyl chloride (3) with acetophenone derivative (4) in presence of sodium methoxide in dry toluene led to the synthesis of substituted β-diketones containing pyrazole moiety (5a-l). All the newly synthesized compounds were confirmed by elemental analysis and IR, 1H, 13C NMR and mass spectral studies. The compounds (5a-l) were evaluated for their antibacterial and antifungal activities.

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Lin, Ying-Tong, Xiao-Wei Yao, Zheng-Wu Luo, et al. "Polyketides with Cardioprotective Bioactivities from Sponge-Associated Fungus Aspergillus giganteus MA46-5." Molecules 30, no. 7 (2025): 1632. https://doi.org/10.3390/molecules30071632.

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One pair of novel enantiomers, gigantdioxin A (+)-1 and B (−)-1, with a skeleton of benzo[d][1,3]dioxin; a new acetophenone gigantone A (3); a known 3-chlorogentisyl alcohol (2), which is the bioprecursor of 1; acetophenone (4); and chromone derivative (5) were obtained from the sponge-associated fungus Aspergillus giganteus MA46-5. Their structures were established by extensive and in-depth spectral analysis, such as UV, 1D and 2D NMR, and HRESIMS. The absolute configurations of (±)-1 were deduced by ORD, chiral separation, and experimental and computational ECD. Meanwhile, we proposed a possible biosynthetic pathway of (±)-1. Fortunately, the pathway was proved by biomimetic synthesis through 2, as a bioprecursor, reacted with n-butyraldehyde. Myocardial protection assays showed that 3 and 4 possessed stronger protective effects than a positive control against myocardial cell H9c2 ischemia–reperfusion injury in low concentrations, and the effect of (−)-1 was almost equal to that of the positive control. Further, we explored the possible mechanism of myocardial protection through network pharmacology. Adenosine A2a receptor (ADORA2A) and serum albumin (ALB) represent potential targets for myocardial protection associated with (−)-1 and 4, respectively. Based on the network pharmacology, we docked the predicted proteins with bioactive compounds using Autodock Vina.

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Ismiyarto, Ismiyarto, Sabirin Matsjeh, and Chairil Anwar. "Synthesis of Chalcone and Flavanone Compound Using Raw Material of Acetophenone and Benzaldehyde Derivative." Indonesian Journal of Chemistry 1, no. 2 (2010): 81–89. http://dx.doi.org/10.22146/ijc.21948.

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Synthesis of flavanoid compounds of chalcone and flavanone groups have been conducted. Flavanoid Is one of the group natural products which is mostly found in plants and have been proved to have physiological activity as drug. In this research, chalcone proup compounds that being synthesized are: chalcone, 3,4-dimethoxychalcone, 2'-hidroxy-3,4-dimethoxychalcone where as compound of flavanone group that being synthesized is 3',4'-dimethoxyflavanone. The synthesis of chalcone group are carried out based on Claisen-Schmidt reaction by using raw material of aromatic aldehydes and aromatic ketones. The synthesis in carried out by stirring at the room temperature using alkali solution as catalyst and ethanol as solvent. The synthesis of 3',4'-dimethoxyflanone is made based on the nucleophilic 1,4 addition of the unsaturated α,β ketone. The synthesis is made by refluxing 2'-hydroxy-3,4-dimethoxychalcone in alkali condition for 12 hours. The identification of flavanoid compound is carried out by using spectroscopic IR, GC-MS and 1H-NMR methods. The result of each synthesis chalcone group are follows: chalcone as yellowish solid with m.p= 50 °C and the yield is 83.39%; 3,4-dimethoxychalcone as yellow solid with m.p= 57°C and the yield is 76.00% ; 2'-hydroxy-3,4-dimethoxychalcone as orange solid with m.p= 90 °C and the yield is 74.29%, for 3',4'-dimethoxyflavanone as pale yellow solid with m.p= 80 °C and the yield is 72.00%.

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Guindy, NM, FM Elzawawy, and DY Sabry. "Photochemical hydrogen formation from a water-soluble acetophenone derivative in presence of colloidal platinum." Journal de Chimie Physique 89 (1992): 629–38. http://dx.doi.org/10.1051/jcp/1992890629.

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Wollenweber, Eckhard, Yoshinori Asakawa, Detlef Schillo, Ulrich Lehmann, and Heidrun Weigel. "A Novel Caffeic Acid Derivative and Other Constituents of Populus Bud Excretion and Propolis (Bee-Glue)." Zeitschrift für Naturforschung C 42, no. 9-10 (1987): 1030–34. http://dx.doi.org/10.1515/znc-1987-9-1004.

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Abstract The bud exudates of Populus nigra, P. trichocarpa, and P. grandidentata × tremuloides were analyzed for the presence of phenolics and flavonoids. A novel natural product, caffeic acid y.y-dimethylallyl ester, was identified from P. nigra, along with further phenolics such as ρ-hydroxy-acetophenone, dimethyl caffeic acid, cinnamoyl cinnamata and vanillin. The flavonoid aglycones correspond to those reported earlier. Propolis samples from the Sonoran Desert were shown to exhibit the flavonoid pattern that is typical for poplar bud exudates, thus confirming this material as the major source for bee-glue. Only a single flavonoid might originate from the leaf exudate of a desert shrub.

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Babu, A. Vasu, A. Rambabu, P. V. Giriprasad, R. Surya Chandra Rao, and B. Hari Babu. "Synthesis of (±)-Pisonivanone and Other Analogs as Potent Antituberculosis Agents." Journal of Chemistry 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/961201.

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A new class of alkylated chalcones and flavanones was synthesised and screened for antituberculosis, antixoidant, and cytotoxic activities. The desired compounds were synthesised using methyl substituted 2-hydroxyacetophenone as a key intermediate. The acetophenone derivative having methyl substitution was prepared in turn from methtylated phloroglucinol by formylation (by Vilsmeier-Haack reaction), followed by reduction with Wolf-Kishnner approach, and finally acetylation was involved. Among 17 compounds, compound5and compound4ainhibitedM. tuberculosisat minimum inhibitory concentration (MIC) in the range between 25 μg/mL and 50 μg/mL. The remaining other 15 compounds also potently inhibitedM. tuberculosisat MIC in range between 50 μg/mL and 100 μg/mL. Some of these compounds also showed moderate antioxidant and cytotoxic activities.

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DELGADO, G. E., P. DELGADO-NIÑO, and J. JAMALIS. "X-RAY POWDER DIFFRACTION DATA FOR A NEW THIOPHENE CHALCONE OBTAINED BY A CLAISEN-SCHMIDT REACTION." Periódico Tchê Química 16, no. 32 (2019): 878–84. http://dx.doi.org/10.52571/ptq.v16.n32.2019.896_periodico32_pgs_878_884.pdf.

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Chalcones and their heterocyclic derivatives have gained considerable importance in recent years due to their wide range of pharmacological properties including anti-AIDS agents, anti-bacterial, anti-malarial, antiinflammatory, anti-leishmanial, anti-oxidant, anti-cancer, anti-tuberculosis anti-microbial activity. These important compounds are conventionally synthesized by Claisen-Schmidt condensation reaction in which aldehyde reacted with acetophenone in the presence of aqueous alkaline bases. Hence the importance of characterizing new derivatives using different techniques both spectroscopic and diffractometric to know their molecular and crystalline structure, but also techniques that allow to study their biological properties to know their possible applications. X-ray powder diffraction is the technique most widely used for the identification of crystalline materials and hence the importance of reporting powder patterns in the Powder Diffraction File database. Therefore, the objective of this investigation is to obtain and reported good quality X-ray powder diffraction data (d-spacing and relative intensity of observed hkl reflections) of the new hetererocyclic chalcone derivative; (E)-3-(5-bromo thiophen-2-yl)-1-(2,5-dichlorothiophen-3-yl)-2-propen-1-one. This new compound was synthesized by Claisen-Schmidt condensation method among a series of thiophene derivative chalcones as potential anti-cancer and anti-microbial agents. The powder pattern was indexed in the monoclinic space group P21/n with unit cell parameters a= 4.0323(7) Å, b= 13.551(3) Å, c= 23.511(5) Å, β= 94.27(1), Z = 4, V= 1281.1(3) Å3, and figures of merit M20= 18.2 and F30= 47.6 (0.0143, 44). All measured lines were indexed and are consistent with the monoclinic space group.

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Vu Quoc, Trung, Duong Tran Thi Thuy, Thuan Dang Thanh, et al. "Some chalcones derived from thiophene-3-carbaldehyde: synthesis and crystal structures." Acta Crystallographica Section E Crystallographic Communications 75, no. 7 (2019): 957–63. http://dx.doi.org/10.1107/s2056989019007503.

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The synthesis, spectroscopic data and crystal and molecular structures of four 3-(3-phenylprop-1-ene-3-one-1-yl)thiophene derivatives, namely 1-(4-hydroxyphenyl)-3-(thiophen-3-yl)prop-1-en-3-one, C13H10O2S, (1), 1-(4-methoxyphenyl)-3-(thiophen-3-yl)prop-1-en-3-one, C14H12O2S, (2), 1-(4-ethoxyphenyl)-3-(thiophen-3-yl)prop-1-en-3-one, C15H14O2S, (3), and 1-(4-bromophenyl)-3-(thiophen-3-yl)prop-1-en-3-one, C13H9BrOS, (4), are described. The four chalcones have been synthesized by reaction of thiophene-3-carbaldehyde with an acetophenone derivative in an absolute ethanol solution containing potassium hydroxide, and differ in the substituent at the para position of the phenyl ring: –OH for 1, –OCH3 for 2, –OCH2CH3 for 3 and –Br for 4. The thiophene ring in 4 was found to be disordered over two orientations with occupancies 0.702 (4) and 0.298 (4). The configuration about the C=C bond is E. The thiophene and phenyl rings are inclined by 4.73 (12) for 1, 12.36 (11) for 2, 17.44 (11) for 3 and 46.1 (6) and 48.6 (6)° for 4, indicating that the –OH derivative is almost planar and the –Br derivative deviates the most from planarity. However, the substituent has no real influence on the bond distances in the α,β-unsaturated carbonyl moiety. The molecular packing of 1 features chain formation in the a-axis direction by O—H...O contacts. In the case of 2 and 3, the packing is characterized by dimer formation through C—H...O interactions. In addition, C—H...π(thiophene) interactions in 2 and C—H...S(thiophene) interactions in 3 contribute to the three-dimensional architecture. The presence of C—H...π(thiophene) contacts in the crystal of 4 results in chain formation in the c-axis direction. The Hirshfeld surface analysis shows that for all four derivatives, the highest contribution to surface contacts arises from contacts in which H atoms are involved.

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Mahmoud, Mohamed E., Maram T. H. Abou Kana, and Ahmed A. Hendy. "Synthesis and implementation of nano-chitosan and its acetophenone derivative for enhanced removal of metals." International Journal of Biological Macromolecules 81 (November 2015): 672–80. http://dx.doi.org/10.1016/j.ijbiomac.2015.08.063.

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Hopf, Henning, Thomas Laue, and Maximilian Zander. "Photochemical and Photophysical Properties of 4- Acyl [2.2] paracyclophanes." Zeitschrift für Naturforschung A 46, no. 9 (1991): 815–18. http://dx.doi.org/10.1515/zna-1991-0911.

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Abstract Photochemical and photophysical properties of 4-benzoyl[2.2]paracyclophane (3) and 4-acetyl[ 2.2]paracyclophane (5) have been studied. In contrast to benzophenone and acetophenone, respectively, the lowest triplet state of 3 and 5 is of the τ, τ*-type. 3 is photochemically reactive. Photoenolization (in solution at lower temperature) is the main reaction pathway while bond fission of an exocyclic C-C bond of the formed photoenol leading to an alkylated open-chain benzophenone derivative takes place to a minor degree. Photoenolization of 3 is the first example of this type of photochemical reaction observed with a cyclophane compound, and at the same time is a novel example of the violation of Bredt's rule. Under certain experimental conditions 3 and 5 may be usable as chiral triplet sensitizers in photochemical reactions

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., Samiya, Supriyo Saha, Vikash Jakhmola, Nidhi Gairola, and Mahipal Singh. "Molecular Docking, Synthesis, Antiproliferative Activity against MCF-7, and In-vitro Alpha Amylase Activities of Newer Generation Pyrimidino Hydroxamic Acid Derivatives." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 14, no. 02 (2024): 649–59. http://dx.doi.org/10.25258/ijddt.14.2.06.

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A set of newer generation pyrimidine hydroxamic acid derivatives were designed, synthesized, and evaluated for antiproliferative activity against breast cancer cell line and in-vitro alpha-amylase activity. The design of the molecules was fully dependent upon the structural features of suberoyl anilide hydroxamic acid. Then all the designed molecules (S1-S100) were docked with 4LXZ HDAC2 enzyme and S1, S2, S16 showed good docking interaction scores as compared to SAHA. The interacting residues of (S1, S2, S16) and 4LXZ showed similar amino acid lining as present in the active site. The synthetic procedure of the molecules (S1, S2, S16) was divided into three parts such as synthesis of chalcone derivative using aromatic aldehyde and acetophenone, the reaction between chalcone and thiourea to form substituted pyrimidine-2-thiol, then finally substituted pyrimidine-2-thiol and 2-chloro-N-hydroxyacetamide reacted in the presence of dimethylformamide to obtain the best-docked molecules. All the molecules showed characteristic peaks in fourier-transform infrared (FTIR), proton nuclear magnetic resonance (1H-NMR) and mass spectrometry with sharp melting points and single peak in thin layer chromatography (TLC) plate. Finally antiproliferative activity against MCF-7 and in-vitro alpha amylase activity data confirmed that S1 was the best molecule among all the synthesized molecules.

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Furuta, Takumi, Toshiyuki Kan, Mitsuru Ueda, Yasuo Hirooka, and Kiyoshi Tanaka. "Synthesis of Diazirine Possessing an Acetophenone Derivative as a Valuable Intermediate for a Flavonoid Photoaffinity Probe." HETEROCYCLES 76, no. 1 (2008): 811. http://dx.doi.org/10.3987/com-07-s(n)4.

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Baiz, Tamam I., and Joseph A. R. Schmidt. "A Discrete Ortho-Lithiated Acetophenone Imine Derivative: Isolation, Characterization, and Synthesis of Group IV Metal Complexes." Organometallics 26, no. 17 (2007): 4094–97. http://dx.doi.org/10.1021/om700530z.

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Dona, Rahma, Jasril, Rudi Hendra, and Neni Frimayanti. "Synthesis and In Vitro Antimalarial Activity of Amino Chalcone Derivative Compounds by Inhibition of Heme Polymerization." Jurnal Sains Farmasi & Klinis 11, no. 2 (2024): 127–35. http://dx.doi.org/10.25077/jsfk.11.2.127-135.2024.

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This study investigated the potential of chalcone derivatives as antimalarial agents. The structures of the chalcone derivatives were designed by including amino substituents on acetophenone and methoxy variants on benzaldehyde. As a result, three amino chalcone derivatives (1-3) were synthesized. The synthesis was conducted by performing the Claisen-Schmidt condensation reaction with 40% NaOH as the base catalyst, resulting in a yield ranging from 66% to 83%. In addition, the structures of the compounds were determined by FTIR, MS, and 1H-NMR spectroscopy techniques, confirming that the compounds possess structures that align with the desired molecular structure. The antimalarial activity test was conducted by inhibiting the process of heme polymerization into hemozoin (β-hematin) in a controlled laboratory setting. This process is one of the key targets of antimalarial medication therapy. Among the compounds, compound 2 exhibited superior antimalarial activity, with an IC50 value of 118.15 μg/mL, in comparison to the positive control hydroxychloroquine sulphate (IC50 value of 184.98 μg/mL). The inhibitory action of heme polymerization in the synthesis of hemozoin was influenced by the location and quantity of methoxy groups in the chalcone molecule, as observed in this work.

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Pungot, Noor Hidayah, Najwa Amira Mohamad Latif, and Nur Ain Nabilah Ash'ari. "Synthesis of 1-acetyl-3,5-diphenyl-1H-pyrazole from Chalcone." ASM Science Journal 14 (April 2, 2021): 1–6. http://dx.doi.org/10.32802/asmscj.2020.629.

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The synthesis of chalcone has drawn tremendous interest over the past years due to its wide applications in the pharmaceutical and biological sectors. Indeed, this compound is reported to possess a broad spectrum of promising bioactivities, including anti-inflammatory, anti-invasive, antioxidant, antitumor and antibacterial properties. In this work, chalcone 3 was synthesised via Claisen-Schmidt condensation by using a common starting material of benzaldehyde 1 and acetophenone 2 in the presence of alcoholic alkaline base. Subsequently, 3,5-diphenyl-2-pyrazoline 4 intermediate was successfully synthesised by reductive amination reaction of 3 with hydrazine hydrate. Thereafter, insertion of acyl subunit at N-1 position of the corresponding amine via 1N-acylation reaction afforded the targeted 1-acetyl-3,5-diphenyl-1H-pyrazole 5 derivative. The structures of all the synthesised compounds were confirmed by elemental analyses, IR, GC-MS and NMR spectra.

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Kiss, László, Heng Li, Hui Yan, and Sándor Kunsági-Máté. "Comparison between Electropolymers of 3,5-Dihydroxybenzoic Acid and 2′,6′-Dihydroxyacetophenone in Dimethyl Sulfoxide and Their Analytical Performance towards Selected Analytes with the Role of the Washing Liquid." Molecules 29, no. 16 (2024): 3972. http://dx.doi.org/10.3390/molecules29163972.

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In the first part of this study, the electrochemical polymerization of two compounds, 3,5-dihydroxybenzoic acid and 2′,6′-dihydroxyacetophenone, was compared in dimethyl sulfoxide solvent on platinum and glassy carbon electrodes. The voltammograms obtained showed remarkable differences between the two monomers and between the two electrode materials. The acetophenone derivative formed electropolymer remnants at the electrodes, while in the case of the benzoic acid derivative, practically no passivation occurred, and the scanning electron microscopic results reinforced this. A few stackings adsorbed only after electropolymerization from a highly concentrated solution of dihydroxybenzoic acid. As a modifying layer on the platinum and glassy carbon electrodes, the prepared films from 2′,6′-dihydroxyacetophenone were tested for tributylamine in acetonitrile and in an aqueous solution of a redox-active compound, hydroquinone, during the stirring of the solution. More stable amperometric current signals could be reached with modified platinum than with glassy carbon, and the significant influence of the organic washing liquid after deposition was established via the study of noise level. In this respect, acetone was the best choice. The amperometric signals with the modified platinum obtained upon the addition of aliquots of the stock solution resulted in a 3.29 μM detection limit.

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