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Journal articles on the topic 'Isoxazole derivatives'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

V S, Anila Kumari, Dr Prasobh G R, and Sheeja Rekha A G. "A Brief Review on Isoxazole Derivatives as Antibacterial Agents." International Journal of Research and Review 9, no. 9 (2022): 321–33. http://dx.doi.org/10.52403/ijrr.20220935.

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Isoxazole compounds exhibit a wide spectrum of targets and broad biological activities. Isoxazole derivatives are still popular scaffolds for the development of new agents with variable biological activities such as antimicrobial, antiviral, anticancer, anti-inflammatory, immunomodulatory, anticonvulsant or antidiabetic properties. The key feature of these heterocycles is that they possess the typical properties of an aromatic system but contain a weak nitrogen-oxygen bond which under certain reaction conditions like reducing or basic conditions is a potential site of ring cleavage. Thus, isox

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2

Ouzounthanasis, Konstantinos A., Jasmina Glamočlija, Ana Ćirić, and Alexandros E. Koumbis. "Studies of the Synthesis of Fused Isoxazoline/Isoquinolinones and Evaluation of the Antifungal Activity of Isoxazole-like Benzamide and Isoquinolinone Hybrids." Molecules 30, no. 3 (2025): 589. https://doi.org/10.3390/molecules30030589.

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Isoxazole derivatives (isoxazoles, isoxazolines, and isoxazolidines) are present in the structure of several natural products and/or pharmaceutically interesting compounds. In this work, a synthetic study for the preparation of fused isoxazoline/isoquinolinone hybrids is presented. The initial approach involving the sequential 1,3-dipolar cycloaddition of nitrile oxides to indenone (to obtain the isoxazoline ring) and a Beckmann rearrangement (to construct the isoquinolinone lactam system) was complicated by the formation of fragmentation products during the latter. Therefore, the desired hybr

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3

Subi, S., S. Viola Rose, and T. F. Abbs Fen Reji. "Synthesis, Characterization, DFT Study, Molecular Modelling and Biological Evaluation of Novel 5-Aryl-3-(pyridine-3-yl)isoxazole Hybrids as Potent Anticancer Agents with Inhibitory Effect on Skin Cancer." Asian Journal of Chemistry 33, no. 10 (2021): 2281–86. http://dx.doi.org/10.14233/ajchem.2021.23335.

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A novel series of pyridinyl isoxazole derivatives was synthesized and characterized by IR, 1H and 13C NMR and high-resolution mass spectrometry. Geometrical and electronic properties of pyridinyl isoxazole derivative was investigated by using B3LYP/6-31G (d,p) basis sets. The HOMO and LUMO analysis was used to determine the charge transfer within the molecule. The pyridinyl isoxazole derivatives exhibited good docking scores against liver cancer 4MMH. The results revealed clearly compound 2b exhibited better radical scavenging ability. Among the synthesized pyridinyl isoxazole derivatives, com

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4

Wang, Haoyu, Yurui Ma, Yifan Lin, et al. "An Isoxazole Derivative SHU00238 Suppresses Colorectal Cancer Growth through miRNAs Regulation." Molecules 24, no. 12 (2019): 2335. http://dx.doi.org/10.3390/molecules24122335.

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Colorectal cancer (CRC) is a leading cause of cancer-related deaths worldwide. Isoxazoline and isoxazole derivatives represent an important class of five-membered heterocycles, which play a pivotal role in drug discovery. In our previous study, we developed a series of isoxazole derivatives with an efficient method. In this study, we evaluated their effects on tumor cell growth. HCT116 cells were treated with isoxazole derivatives; an cholecystokinin octapeptide (CCK-8) assay was used to calculate the IC50 (half maximal inhibitory concentration) of each derivative. Compound SHU00238, which was

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5

Thirunarayanan, G., and V. Sathiyendiran. "Synthesis, Pharmacological and Insect Antifeedant Activities of some 3-(2-Naphthyl)-5-(Substituted Phenyl)-4,5-Dihydroisoxazoles." International Letters of Chemistry, Physics and Astronomy 49 (April 2015): 1–14. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.49.1.

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Totally thirty one 3,5-substituted aryl 4,5-dihydro isoxazole derivatives including 3-(2-naphthyl)-5-(substituted phenyl)-4,5-dihydroisoxazole have been synthesized by fly-ash:H2SO4 catalyzed cyclization of hydroxylamine hydrochloride and aryl chalcones under solvent-free conditions. The yields of the isoxazoles are more than 94%. The synthesized isoxazole were characterized by their physical constants and spectral data. The antimicrobial, antioxidant and insect antifeedant activities of the synthesized isoxazoles have been evaluated using a variety of bacterial and fungal species, DPPH radica

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6

Thirunarayanan, G., and V. Sathiyendiran. "Synthesis, Pharmacological and Insect Antifeedant Activities of some 3-(2-Naphthyl)-5-(Substituted Phenyl)-4,5-Dihydroisoxazoles." International Letters of Chemistry, Physics and Astronomy 49 (April 7, 2015): 1–14. http://dx.doi.org/10.56431/p-g0r04d.

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Totally thirty one 3,5-substituted aryl 4,5-dihydro isoxazole derivatives including 3-(2-naphthyl)-5-(substituted phenyl)-4,5-dihydroisoxazole have been synthesized by fly-ash:H2SO4 catalyzed cyclization of hydroxylamine hydrochloride and aryl chalcones under solvent-free conditions. The yields of the isoxazoles are more than 94%. The synthesized isoxazole were characterized by their physical constants and spectral data. The antimicrobial, antioxidant and insect antifeedant activities of the synthesized isoxazoles have been evaluated using a variety of bacterial and fungal species, DPPH radica

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7

Arshad, Nasima, Yasir Mehmood, Hammad Ismail, et al. "Newly synthesized sulfonamide derivatives explored for DNA binding, enzyme inhibitory, and cytotoxicity activities: a mixed computational and experimental analyses." RSC Advances 14, no. 47 (2024): 35047–63. http://dx.doi.org/10.1039/d4ra06412g.

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This work reports synthesis, characterization, DNA, enzyme binding and cytotoxicity activity of three 4-((3-arylthiazolo[3,4-d]isoxazol-5-yl)amino)benzene sulfonamide derivatives with a thaizaole(3,4-d)isoxazole-based fused ring heterocyclic system.

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8

Sharma, Aruna, Anjali Yadav, Hardik Pathak, Bhawana Jangir, and Rahul Goel. "Effective synthesis and pharmacological evaluation of 1,2,4-triazolo-isoxazole and 1,2,4-triazolo-pyrazole scaffolds." Research Journal of Chemistry and Environment 29, no. 5 (2025): 77–82. https://doi.org/10.25303/295rjce077082.

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Five-membered heteroaromatic compounds like pyrazoles and isoxazoles are significant for the pharmaceutical sector and material research, becoming more significant in drug research, cosmetics as well as in the creation of agricultural products. 1,2,4-triazolo fused isoxazole derivatives (3a-f) were synthesized from reaction between intermediate chal cone-1,2,4-triazolo-1,5-benzodiazepine derivatives 2af with hydroxyl amine hydrochloride. 1,2,4-triazolo fused pyrazole derivatives (3a-f and 4a-f) were prepared from reaction between chalcone derivatives 2a-f with hydrazine hydrate and its phenyl

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9

S. Abibindhu, Smitha Nair, and C. Kannan. "SYNTHESIS AND ANTI-INFLAMMATORY, ANTIOXIDANT STUDIES OF NOVEL CHALCONES-BASED ISOXAZOLE DERIVATIVES." RASAYAN Journal of Chemistry 15, no. 04 (2022): 2661–65. http://dx.doi.org/10.31788/rjc.2022.1547023.

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Our previous work identified various novel Chalcones (I-III) produced by mixing the equimolar amount of Ferrocene aldehyde and different substituted acetophenones which has a strong base. Hence, in the present study, novel various Chalcones (I-III) were treated with hydroxylamine hydrochloride to form various Isoxazoles (Ic-IIIc). The synthesized novel chalcone-based Isoxazole derivatives were determined by spectroscopic techniques such as1H,13C-NMR, FT-IR,and UV. Further, these products were evaluated for antimicrobial studies and antioxidant susceptibilities through DPPH radical scavenging m

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10

Al-Omran, Fatima, and Adel A. El-Khair. "Studies with 2-(acetonylthio)benzothiazole. New routes to isoxazoles, isoxazolo[3,4-b]pyridines, pyrazolo[1,5-a]pyrimidines, pyridines and quinolizines." Journal of Chemical Research 2009, no. 7 (2009): 433–36. http://dx.doi.org/10.3184/030823409x464412.

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Derivatives of isoxazole, isoxazolo[3,4- b]pyridine, pyrazolo-[1,5- a]pyrimidine and pyridin-2(1 H)-one incorporating a benzothiazole-2-thio residue have been synthesised. The structures of these newly synthesised compounds are characterised by elemental analysis, IR, 1H and 13C NMR, NOE and MS.

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11

Duc, Dau Xuan, and Vo Cong Dung. "Recent Progress in the Synthesis of Isoxazoles." Current Organic Chemistry 25, no. 24 (2021): 2938–89. http://dx.doi.org/10.2174/1385272825666211118104213.

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Isoxazole derivatives are aromatic five-membered ring heterocyclic compounds with one oxygen atom and one nitrogen atom at adjacent positions. These compounds have a broad spectrum of applications in medicinal chemistry, such as antimicrobial, anticancer, antitumor, antitubercular, analgesic, anti-inflammatory, antidepressant, and anticonvulsant activities and some of them are well-known drugs for the treatment of various diseases in the market. The use of this class of compounds in agriculture as herbicides, insecticides have been widely reported. In organic materials, these compounds have be

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12

Antonini, Cosimo, Franca M. Cordero, and Fabrizio Machetti. "5-(Benzoyloxymethyl)isoxazole-3-carboxylic Acid Ethyl Ester." Molbank 2024, no. 1 (2024): M1762. http://dx.doi.org/10.3390/m1762.

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We describe here the palladium hydrogenation of ethyl 5-(benzoyloxymethyl)isoxazole-3-carboxylate. The presence of two reducible sites in the molecule, namely the benzylic-like position and the isoxazole N–O bond, creates a possible competition. The results show that under the applied conditions, ethyl (Z)-2-amino-4-oxo-2-pentanoate is obtained as the only product. Accordingly, a domino process occurs, consisting of deoxygenation to the 5-methylisoxazole derivative followed by reductive opening of the isoxazole ring. The isoxazole substrate was prepared by NaOH-catalyzed cycloaddition-condensa

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13

Beccalli, E. M., A. Marchesini, and T. Pilati. "Oxazolo[4,5-d]isoxazole Derivatives and 3,4-Disubstituted Isoxazoles from Isoxazol-5(4H)-ones." Synthetic Communications 23, no. 5 (1993): 685–702. http://dx.doi.org/10.1080/00397919308009828.

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14

V, Kumar, and Rao CMMP. "Pharmacological Screening of Some Novel 3,5-Disubstituted Isoxazoles Derivatives of Dibromochalcones." INTERNATIONAL JOURNAL OF DRUG DELIVERY TECHNOLOGY 14, no. 04 (2024): 1130–38. https://doi.org/10.25258/ijddt.14.4.30.

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Background: The preparation of some novel 3, 5-disubstituted isoxazole derivatives of dibromochalcones is encouraged by the study. When hydroxylamine hydrochloride and α-β chalcone dibromide combine, a new technique for synthesizing 3,5-disubstituted isoxazoles is produced. Bromine or N-BromoSuccinimide can be used to produce compounds with low polarity like carbon tetrachloride, chloroform and dichloromethane; however the product obtained are very little. Tetrabutylammonium tribromide (TBABr3), thus, induces chalcones to bromate regioselectively and produces a high yield without polymerisatio

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15

Fišera, Lubor, and Peter Oravec. "Stereoselectivity of cycloadditions of arylnitrile oxides to 5-alkoxy-2(5H)-furanone." Collection of Czechoslovak Chemical Communications 52, no. 5 (1987): 1315–24. http://dx.doi.org/10.1135/cccc19871315.

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1,3-Dipolar cycloaddition of arylnitrile oxides to 5-alkoxy-2(5H)-furanones (II) and 5-hydroxy-2(5H)-furanone leads regiospecifically to 4-oxo-3a,4,6,6a-tetrahydrofuro[3,4-d]isoxazole derivatives IIIa-IIIj. The alkoxy derivatives give exclusively products of exo-configuration (III), whereas the hydroxy compound affords a 52 : 48 mixture of both diastereoisomers IIIj and IVj. Reaction of III with ammonia furnished diastereoisomeric tetrahydropyrrolo[3,4-d]isoxazoles V and VI, reaction with hydrazines led to hexahydroisoxazolo[4,5-d]pyridazin-7-one derivatives VII.

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16

Ahmed, Sarbast, Hayman Abdulrahman, Faiq Hussain, Hiwa Ahmad, Idrees Qader, and Hemn Qader. "Synthesis, characterization and biological activity of some isoxazole derivatives via 1,3-dipolar cycloaddition reaction of nitrile oxide." Zanco Journal of Medical Sciences 29, no. 1 (2025): 137–53. https://doi.org/10.15218/zjms.2025.015.

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Background and objective: Isoxazoles are significant heterocyclic products that are used in various applications in the field of medicinal chemistry. Along with prescription drugs, a variety of bioactive pharmaceutical substances, such as valdecoxib, leflunomide, and danazol, include the isoxazole core. The present work aimed to synthesize and test the antibacterial, antioxidant, and antifungal activities combined with the theoretical investigations. Methods: Various 2,4-disubstituted isoxazoles have been synthesized through a 1,3-dipolar cycloaddition reaction via nitrile oxide. The structure

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17

Sangale, Shital S., Priyanka S. Kale, Rachana B. Lamkane, Ganga S. Gore, Priyanka B. Parekar, and Shivraj S. Shivpuje. "Synthesis of Novel Isoxazole Derivatives as Analgesic Agents by Using Eddy’s Hot Plate Method." South Asian Research Journal of Pharmaceutical Sciences 5, no. 01 (2023): 18–27. http://dx.doi.org/10.36346/sarjps.2023.v05i01.002.

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The Isoxazole ring system belongs to a much studied class of compound. In the last few decades, the chemistry of Isoxazoles and their fused heterocyclic derivatives have received considerable attention owing to their significant and effective biological activity. The present study aimed to design and synthesize novel derivatives of Isoxazole from 4-methoxy aniline gives N-(4-methoxyphenyl) acetamide which was hydrolysis with sodium hydroxide and treated aromatic aldehydes yields resultant compound N-(4-methoxyphenyl) 3-phenyl propanamide (BSM-IIIA-IIIJ). Title compound were synthesized and the

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18

Gonçalves, Itamar L., Rafaela R. da Rosa, Vera L. Eifler-Lima, and Aloir A. Merlo. "The use of isoxazoline and isoxazole scaffolding in the design of novel thiourea and amide liquid-crystalline compounds." Beilstein Journal of Organic Chemistry 16 (February 6, 2020): 175–84. http://dx.doi.org/10.3762/bjoc.16.20.

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A series of novel thiourea and amide liquid crystals containing 5-membered isoxazoline and isoxazole rings were synthetized and the liquid crystal properties studied. Thioureas were obtained using a condensation reaction of benzoyl chlorides, arylamines and ammonium thiocyanate. The amides, on the other hand, were the byproduct of a quantitative reaction which used potassium cyanate as the starting material. Thiourea and amide derivatives were predominantly SmA mesophase inductors. A nematic mesophase was observed only for thioureas and amides containing an isoxazole ring. Additionaly, the liq

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19

Kiyani, Hamzeh, and Asiyeh Mosallanezhad. "Sulfanilic Acid-catalyzed Synthesis of 4-arylidene-3-substituted isoxazole-5(4H)-ones." Current Organic Synthesis 15, no. 5 (2018): 715–22. http://dx.doi.org/10.2174/1570179415666180423150259.

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Aim and Objective: In recent studies, chemistry of heterocyclic compounds, especially isoxazoles, has been widely considered by organic chemistry researchers because they have been found in many molecules, including naturally occurring bioactive compounds, pharmaceuticals, and agrichemicals. Isoxazol- 5(4H)-ones and their derivatives, on the other hand, have significant biological properties can be mentioned as examples of antibacterial, anti-inflammatory, antifungal, anticancer, analgesic, fungicidal, and insecticidal activities. Therefore, the development of ecofriendly methods, such as thre

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20

Hodyna, Diana M., Oleksandr V. Pavliuk, Maria M. Baran, Vitaliy O. Yevdokymenko, Vasyl V. Kovalishyn, and Larysa O. Metelytsia. "Isoxazole-containing sulfanilamides as new antibacterial agents: in silico study, synthesis and in vitro evaluation." Ukr. Bioorg. Acta 2022, Vol. 17, N2 17, no. 2 (2022): 23–30. http://dx.doi.org/10.15407/bioorganica2022.02.023.

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The QSAR models previously created by the OCHEM web platform were used for the research and design of novel isoxazole derivatives as antimicrobial agents. Based on the created virtual set of promising isoxazole derivatives, a number of potential antibacterial agents were selected for synthesis and further research. A convenient synthetic sequence for obtaining initial isoxazole-containing sulfonylamides and preparative methods for the synthesis of target sulfonylamides of the isoxazole series, in particular, using ring-closing metathesis reactions, were worked out. The results of in vitro anti

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21

Kosaraju Lahari and Raja Sundararajan. "Design, Synthesis, Characterisation & Anticonvulsant Activities of Novel Heterocyclic Substituted Isatin Derivatives." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (2020): 6351–62. http://dx.doi.org/10.26452/ijrps.v11i4.3392.

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Twelve new isoxazole/pyrazole/pyrimidine substituted 5-nitrosation analogues were designed according to the requirements of the anticonvulsant drugs pharmacophore model and synthesised from indole-2,3-dione. Entire prepared compounds chemical structures were established from its IR, proton-NMR, Mass spectrum & microanalysis data. Anticonvulsant potency of final isatin analogues was assessed by MES technique & sc PTZ technique. Besides rotarod test was used to assess the neurotoxicity of all potent title analogues. Title compounds exhibited a varying degree of anticonvulsant potency ran

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22

Qiu, Dengxu, Chenhui Jiang, Pan Gao, and Yu Yuan. "Lewis acid-promoted direct synthesis of isoxazole derivatives." Beilstein Journal of Organic Chemistry 19 (October 16, 2023): 1562–67. http://dx.doi.org/10.3762/bjoc.19.113.

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Isoxazole derivatives were synthesized via a one-pot method utilizing 2-methylquinoline derivatives as template substrates, sodium nitrite as a nitrogen-oxygen source, and solely using aluminum trichloride as the additive. This approach circumvents the need for costly or highly toxic transition metals and presents a novel pathway for the synthesis of isoxazole derivatives.

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23

Herbert, C. G., and R. G. Bass. "Preparation and characterization of poly(arylene ether isoxazole)s by fluoride ion-mediated aromatic nucleophilic displacement reactions." High Performance Polymers 6, no. 4 (1994): 303–19. http://dx.doi.org/10.1088/0954-0083/6/4/002.

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As part of a continuing effort to prepare novel thermally stable high-performance polymers, poly(arylene ether isoxazole)s have been prepared by fluoride ion-catalysed aromatic nucleophilic substitution reactions with bis(trimethylsiloxyphenyl) isoxazoles and activated bisarylhalides in diphenyl sulphone. Initial investigations involving the preparation of these materials with isoxazole bisphenols and activated bisarylhalides in the presence of potassium carbonate indicated that, under reaction conditions necessary to prepare high-molecular-weight materials, the isoxazole monomer was converted

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24

Komshina, Lyudmila, Aleksandr Kotov, Mariya Blyumina, and Elena Vasil'eva. "Synthesis of sulfonylamides containing an isoxazole moiety." From Chemistry Towards Technology Step-By-Step 5, no. 2 (2024): 109–26. http://dx.doi.org/10.52957/2782-1900-2024-5-2-109-126.

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The authors obtained a number of new sulfonylamides with isoxazole moiety by sulfonyl chlorination of bicyclic systems containing isoxazole heterocycle and interaction of the obtained sulfonyl chlorides with amino compounds. The authors also obtained isoxazole derivatives containing a sulfogroup in the isoxazole ring by sulfonyl chlorination of 3-aryl-5-N-acylaminoisoxazoles.

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25

BECCALLI, E. M., A. MARCHESINI, and T. PILATI. "ChemInform Abstract: Oxazolo(4,5-d)isoxazole Derivatives and 3,4-Disubstituted Isoxazoles from Isoxazol-5(4H)-ones." ChemInform 24, no. 26 (2010): no. http://dx.doi.org/10.1002/chin.199326129.

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26

Chukanov, N. V., S. A. Popov, G. V. Romanenko, and V. A. Reznikova. "Transformation of 1,2,3,7a-tetrahydroimidazo[1,2-b]isoxazole derivatives into isoxazoles." Russian Chemical Bulletin 56, no. 6 (2007): 1227–33. http://dx.doi.org/10.1007/s11172-007-0185-y.

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27

Akishina, E. A., E. A. Dikusar, S. K. Petkevich, and V. I. Potkin. "Synthesis of isoxazole and isothiazole derivatives of curcumin." Proceedings of the National Academy of Sciences of Belarus, Chemical Series 56, no. 2 (2020): 187–91. http://dx.doi.org/10.29235/1561-8331-2020-56-2-187-191.

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Curcumin is a chemical compound with antioxidant properties as well as strong anti-inflammatory, antiviral, analgesic, antimicrobial and antitumor effect, contained in the tuberous rhizomes of the turmeric plant (Curcuma longa). Curcumin derivatives are being intensively studied as potential drugs – antitumor drugs for the treatment of certain forms of cancer. The presence of reactive functional groups makes curcumin a convenient starting compound for the further chemical modification. The esters of curcumin and 5-phenylisoxazole-3-carboxylic acid, 5-(p-tolyl)isoxazole-3-carboxylic acid, 4,5-

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Liu, Xin-Hua, Bao-An Song, Pinaki S. Bhadury, et al. "Novel 5-(3-(Substituted)-4,5-dihydroisoxazol-5-yl)-2-methoxyphenyl Derivatives: Synthesis and Anticancer Activity." Australian Journal of Chemistry 61, no. 11 (2008): 864. http://dx.doi.org/10.1071/ch07395.

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Thirty novel 5-(3-(substituted phenyl)-4,5-dihydroisoxazol-5-yl)-2-methoxyphenyl derivatives were synthesized and evaluated for their antitumour activity. The bioassays showed that the 2-fluorobenzoyl derivative 6ai, the 4-trifluoromethylbenzoyl derivative 6ah, and the 3-trifluoromethyl isoxazole derivatives (6ch and 6ci) were highly effective against PC-3 cells. The IC50 values of 6ah and 6ai against PC-3 cells were 1.5 and 1.8 μg mL–1, respectively.

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Vasilenko, Dmitry A., Nadezhda S. Temnyakova, Sevastian E. Dronov, et al. "5-Nitroisoxazoles in SNAr Reactions: A Novel Chemo- and Regioselective Approach to Isoxazole-Based Bivalent Ligands of AMPA Receptors." International Journal of Molecular Sciences 24, no. 22 (2023): 16135. http://dx.doi.org/10.3390/ijms242216135.

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An efficient regioselective approach to novel functionalized bis(isoxazoles) with a variety of aromatic and aliphatic linkers was elaborated, based on the heterocyclization reaction of electrophilic alkenes under the treatment with tetranitromethane-triethylamine complex affording 3-EWG-5-nitroisoxazoles. The subsequent SNAr reactions of 5-nitroisoxazoles with various O,O-, N,N- and S,S-bis(nucleophiles) provide a wide range of bis(isoxazole) derivatives in good isolated yields. Employing an elaborated method, a series of novel bis(3-EWG-isoxazoles) as the promising allosteric modulators of AM

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Carrasco, Fernando, Wilfredo Hernández, Oscar Chupayo, et al. "Phenylisoxazole-3/5-Carbaldehyde Isonicotinylhydrazone Derivatives: Synthesis, Characterization, and Antitubercular Activity." Journal of Chemistry 2021 (October 31, 2021): 1–14. http://dx.doi.org/10.1155/2021/6014093.

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Eight new phenylisoxazole isoniazid derivatives, 3-(2′-fluorophenyl)isoxazole-5-carbaldehyde isonicotinylhydrazone (1), 3-(2′-methoxyphenyl)isoxazole-5-carbaldehyde isonicotinylhydrazone (2), 3-(2′-chlorophenyl)isoxazole-5-carbaldehyde isonicotinylhydrazone (3), 3-(3′-clorophenyl)isoxazole-5-carbaldehyde isonicotinylhydrazone (4), 3-(4′-bromophenyl)isoxazole-5-carbaldehyde isonicotinylhydrazone (5), 5-(4′-methoxiphenyl)isoxazole-3-carbaldehyde isonicotinylhydrazone (6), 5-(4′-methylphenyl)isoxazole-3-carbaldehyde isonicotinylhydrazone (7), and 5-(4′-clorophenyl)isoxazole-3-carbaldehyde isonico

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Muthusamy, Selvaraj, Soo Min Lee, Minghua Huang, et al. "Isoxazoline, Isoxazole, and Oxadiazole Derivatives as M1Muscarinic Acetylcholine Receptor Agonists." Bulletin of the Korean Chemical Society 37, no. 7 (2016): 1020–28. http://dx.doi.org/10.1002/bkcs.10811.

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Visweswara, Rao Ch, Ramanaiah M., and Lakshman Shaik. "Effect of Palladium acetate as Catalyst on the Synthesis of Novel Isoxazole Derivatives incorporating Carbazole Moiety." Research Journal of Chemistry and Environment 27, no. 11 (2023): 24–34. http://dx.doi.org/10.25303/2711rjce024034.

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Isoxazole and carbazole derivatives have a wide range of biological activity and are of high interest to medicinal chemists. We report the synthesis and characterization of a series of novel isoxazole derivatives which were synthesized by linking the isoxazole moiety to the carbazole nucleus. The process of synthesis and the steps involved in the synthesis of these novel derivates are described in detail in this study. We confirmed the structures of the novel compounds by 1H NMR, 13C NMR, LCMS spectral data as well as by elemental analysis. The antimicrobial activity of newly synthesized compo

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Qneibi, Mohammad, Mohammed Hawash, Sosana Bdir, et al. "Regulating AMPA Receptors with Isoxazole-4-Carboxamide Derivatives: An Electrophysiological Study." Journal of Xenobiotics 15, no. 2 (2025): 40. https://doi.org/10.3390/jox15020040.

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Isoxazole carboxamide derivatives are intriguing modulators of ionotropic glutamate receptors; more specifically, their prospective analgesic activities based on non-opioid pathways have sparked widespread research. α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, especially Ca2+-permeable subtypes that are highly expressed in the spinal dorsal horn, play a critical role in nociceptive transmission and inflammatory pain. Herein, the neuromodulatory effects of these derivatives on AMPA receptor activity have been studied, focusing on their potential as modulators of AMPA r

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Mączyński, Marcin, Andrzej Regiec, Paulina Płoszaj, Miroslawa Kacaniova, and Agnieszka Piwowar. "EVALUATION OF ANTIBACTERIAL ACTIVITY 5-AMINO-3-METHYLISOXAZOLE-4-CARBOHYDRAZIDE AND 5-AMINOISOXAZOLE[5,4-d]PYRIMIDIN-4-ONE DERIVATIVES." Acta Poloniae Pharmaceutica - Drug Research 80, no. 1 (2023): 79–90. http://dx.doi.org/10.32383/appdr/162790.

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Searching for new compounds with specific biological activity in relation to various bacterial strains due to the increasing number of bacterial infections and the frequently developing antimicrobial resistance (AMR) is a significant problem in healthcare. Based on previous promising research related to the activity of isoxazole-4-carbohydrazide derivatives, we currently examined different substituted isoxazole-4-carbohydrazide derivatives in vitro against a panel of bacterial strains. In this work we evaluated antibacterial activity of 30 derivatives, previously described as mildly antimycoba

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Zuccato, Cristina, Lucia Carmela Cosenza, Chiara Tupini та ін. "New Synthetic Isoxazole Derivatives Acting as Potent Inducers of Fetal Hemoglobin in Erythroid Precursor Cells Isolated from β-Thalassemic Patients". Molecules 29, № 1 (2023): 8. http://dx.doi.org/10.3390/molecules29010008.

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Induction of fetal hemoglobin (HbF) is highly beneficial for patients carrying β-thalassemia, and novel HbF inducers are highly needed. Here, we describe a new class of promising HbF inducers characterized by an isoxazole chemical skeleton and obtained through modification of two natural molecules, geldanamycin and radicicol. After preliminary biological assays based on benzidine staining and RT-qPCR conducted on human erythroleukemic K562 cells, we employed erythroid precursors cells (ErPCs) isolated from β-thalassemic patients. ErPCs weretreated with appropriate concentrations of isoxazole d

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Alshamari, Asma, Mahmoud Al-Qudah, Fedaa Hamadeh, Lo’ay Al-Momani, and Sultan Abu-Orabi. "Synthesis, Antimicrobial and Antioxidant Activities of 2-Isoxazoline Derivatives." Molecules 25, no. 18 (2020): 4271. http://dx.doi.org/10.3390/molecules25184271.

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A series of derivatives of trans-3-(2,4,6-trimethoxyphenyl)4,5-dihydroisoxazolo-4,5-bis[carbonyl-(4′phenyl)thiosemicarbazide (9) and of trans-3-(2,4,6-trimethoxyphenyl)-4,5-dihydro isoxazolo-4,5-bis(aroylcarbohydrazide) (10a–c) were synthesized from trans-3-(2,4,6-trimethoxyphenyl)-4,5-dihydro-4,5-bis(hydrazenocarbonyl)isoxazole (8). The structures of the compounds were elucidated by both elemental and spectral (IR, NMR, and MS) analysis. Compound 9 shows activity against some bacterial species. No antibacterial activities were observed for compounds 10a–c. The antioxidant activity of the new

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Ismailov, V. M., M. M. Kantaeva, I. A. Mamedov, and N. N. Yusubov. "Synthesis of new isoxazole derivatives." Russian Journal of Organic Chemistry 40, no. 12 (2004): 1826–27. http://dx.doi.org/10.1007/s11178-005-0108-z.

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Chavan, Uma, Kratika Daniel, and Neetesh Kumar Jain. "To Synthesize Naphthalene Derivatives Having Isoxazole Central Core as Anti- Microbial Agents." International Journal of Medical Sciences and Pharma Research 8, no. 2 (2022): 60–64. http://dx.doi.org/10.22270/ijmspr.v8i2.40.

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The presence of heterocycles such as pyrrole, thiazole, oxazole, furane, imidazole, and isoxazole and pyrimidine nucleus as central scaffold is a common feature in the chemical structure of several antimicrobial agents. So the aim has been designed to synthesize the molecule having Naphthalene ring in one of diaryl having isoxazole as pharmacophoric heterocyclic moiety for synthesis of safer anti-microbial agents. Keywords: Naphthalene, isoxazole, anti-microbial agents.

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Sydhulua, Rachakonda, and Yerrabelly Hemasria. "Synthesis of Novel Isoxazoline/Isoxzolyl Pyrano Heterocyclic Annulated Flavones." Asian Journal of Chemistry 35, no. 3 (2023): 624–28. http://dx.doi.org/10.14233/ajchem.2023.27286.

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The synthesis of new isoxazoline/isoxazole pyrano fused flavone derivatives from 6-hydroxy 5-formyl flavone via in situ generation of nitrile oxide from aldoxime using ceric ammonium nitrate (CAN) as an oxidant followed by intramolecular cycloaddition reaction at olefin/alkyne functions is reported in high yields. The reaction involves regio selective annulation at C5/C6 position in preference to the C6/C7 position of flavones. All the synthesized compounds were successfully characterized by IR, 1H NMR, 13C NMR and ESI-MS.

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Feriotto, Giordana, Paolo Marchetti, Riccardo Rondanin, et al. "Cytotoxicity of Isoxazole Curcumin Analogs on Chronic Myeloid Leukemia-Derived K562 Cell Lines Sensitive and Resistant to Imatinib." International Journal of Molecular Sciences 24, no. 3 (2023): 2356. http://dx.doi.org/10.3390/ijms24032356.

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Despite curcumin (CUR) inhibiting cell proliferation in vitro by activating apoptotic cell death, its use in pharmacological therapy is hampered by poor solubility, low stability in biological fluids, and rapid removal from the body. Therefore, CUR-derivatives with better biological and chemical–physical characteristics are needed. The bis-ketone moiety of CUR strongly influences its stability in slightly alkaline solutions such as plasma. Here, we considered its replacement with isoxazole, beta-enamine, or oxime groups to obtain more stable derivatives. The evaluation of the chemical–physical

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Limbadri, P., and Y. Hemasri. "Synthesis of a New Class of Functionalized Isoxazole/Isoxazoline Styrylchromone Derivatives." Russian Journal of Organic Chemistry 61, no. 2 (2025): 312–19. https://doi.org/10.1134/s1070428025020162.

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Yang, Zaibo, Pei Li, and Xiuhai Gan. "Novel Pyrazole-Hydrazone Derivatives Containing an Isoxazole Moiety: Design, Synthesis, and Antiviral Activity." Molecules 23, no. 7 (2018): 1798. http://dx.doi.org/10.3390/molecules23071798.

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In this study, a series of novel pyrazole-hydrazone derivatives containing an isoxazole moiety were synthesized. Antiviral bioassays indicated that some of the title compounds exhibited better in vivo antiviral activities against tobacco mosaic virus (TMV). In particular, compounds 6a, 6c and 6q exhibited the best curative activity, protection activity, and inactivation activity against TMV, respectively, which were superior to those of Ningnanmycin. This study demonstrated that this series of novel pyrazole-hydrazone derivatives containing an isoxazole amide moiety could effectively control T

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Kazak, D. V., Е. А. Dikusar, E. A. Akishina, R. S. Alexeev, N. A. Bumagin, and V. I. Potkin. "Synthesis and properties of esters and amides of pyridine- and 1,2-azolcarbonic acids." Proceedings of the National Academy of Sciences of Belarus, Chemical Series 57, no. 2 (2021): 185–94. http://dx.doi.org/10.29235/1561-8331-2021-57-2-185-194.

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Based on esters of nicotinic and isonicotinic acids with hydroxybenzaldehydes, a series of functionally substituted derivatives containing isoxazole and isothiazole heterocycles in the molecule have been synthesized. Azomethines were obtained by condensation of nicotinates and isonicotinates with p-bromoaniline and m-aminophenol, which have been reduced with sodium triacetoxyborohydride to give the corresponding amines. Acylation of amino derivatives of nicotinates and isonicotinates with 5-arylisoxazole- and 4,5-dichloroisothiazolecarbonyl chlorides leads to the esters and amides with isoxazo

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BinSabt, Mohammad H., Abdulrahman Alazemi, Hamad M. Al-Matar, Alan L. Balch, and Mona A. Shalaby. "Pyrazole-, isoxazole- and pyrrole-ring fused derivatives of C₆₀: synthesis and electrochemical properties as well as morphological characterization." New Journal of Chemistry 46, no. 14 (2022): 6663–69. http://dx.doi.org/10.1039/d2nj00421f.

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Batchelor, Kevin J., W. Russell Bowman, Roy V. Davies, Michael H. Hockley, and David J. Wilkins. "Regioselective Addition of Grignard Reagents to Isoxazole-4,5-dicarboxylate Esters." Journal of Chemical Research 23, no. 7 (1999): 428–29. http://dx.doi.org/10.1177/174751989902300712.

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Regioselective mono-addition of a range of Grignard reagents with the 5-esters of 3-methylisoxazole-4,5-diesters affords 5-keto derivatives instead of tertiary alcohols which is explained by the complexing ability of the isoxazole oxygen atom and by the electron withdrawing effect of the isoxazole ring.

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Vashisht, Ketan, Pooja Sethi, Anshul Bansal, et al. "Synthesis, characterization of isoxazole derivatives and evaluation of their antibacterial, antioxidant and anticancer activity." European Journal of Clinical and Experimental Medicine 22, no. 2 (2024): 376–87. http://dx.doi.org/10.15584/ejcem.2024.2.25.

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Introduction and aim. The synthesis of heterocyclic compounds containing oxygen and nitrogen is profoundly intriguing due to their mechanistic implications in both research and development within organic chemistry and drug discovery. The primary aim of this study is to fabricate a range of pharmacologically active drugs containing the isoxazole moiety. Material and methods. The synthesis of new derivatives of isoxazole was achieved through a one-pot condensation reaction of 2-[(Substituted phenyl)hydrazono]malononitrile (1) and 3-[(Substituted phenyl)azo]-2,4-Pentanedione (2) with sodium aceta

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Bhadani, V. N., H. D. Purohit, and Dipak M. Purohit. "Synthesis and Biological Screening of 3-Aryl-5-[(4′-Difluoromethoxy)(3′-Hydroxy)Phenyl]-4,5-Dihydro Isoxazole." International Letters of Chemistry, Physics and Astronomy 47 (February 2015): 133–38. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.47.133.

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Isoxazoline derivatives shows various types of therapeutic activities like antimicrobial[1], anti-inflammatory[2], anticonvulsant[3], Hypoglycemic[4] etc. getting to synthesized in view of 3-Aryl-5-[(4′-difluoromethoxy)(3′-hydroxy)phenyl]-4,5-dihydro isoxazole (4a-4i) have been synthesized. All the newly synthesized compounds were screened for their antibacterial activity against S. aureus, M. luteus (Gram-positive bacteria), E. coli, S. thyphi (Gram-negative bacteria) and antifungal activity against Candida albicans (Fungi). The biological activities (MIC) of the synthesized compounds were co

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Bhadani, V. N., H. D. Purohit, and Dipak M. Purohit. "Synthesis and Biological Screening of 3-Aryl-5-[(4′-Difluoromethoxy)(3′-Hydroxy)Phenyl]-4,5-Dihydro Isoxazole." International Letters of Chemistry, Physics and Astronomy 47 (February 24, 2015): 133–38. http://dx.doi.org/10.56431/p-672i37.

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Isoxazoline derivatives shows various types of therapeutic activities like antimicrobial[1], anti-inflammatory[2], anticonvulsant[3], Hypoglycemic[4] etc. getting to synthesized in view of 3-Aryl-5-[(4′-difluoromethoxy)(3′-hydroxy)phenyl]-4,5-dihydro isoxazole (4a-4i) have been synthesized. All the newly synthesized compounds were screened for their antibacterial activity against S. aureus, M. luteus (Gram-positive bacteria), E. coli, S. thyphi (Gram-negative bacteria) and antifungal activity against Candida albicans (Fungi). The biological activities (MIC) of the synthesized compounds were co

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Kumar Singh, Amrendra, Ram Naresh Yadav, and Vijay Pratap Singh. "Synthesis and Characterization of Sugar Derived Novel Bioactive Isoxazole Derivatives." International Journal of Science and Research (IJSR) 12, no. 11 (2023): 1610–13. http://dx.doi.org/10.21275/sr231125003436.

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P., RAJANI, ASHOK D., and N. SARMA P. "Synthetic Experiments on Pongamol." Journal of Indian Chemical Society Vol. 68, Jan 1991 (1991): 52–55. https://doi.org/10.5281/zenodo.5968139.

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Department of Chemistry, Osmania University, Hyderabad-500 007 <em>Manuscript received 5 October 1990, accepted 14 January 1991</em> A number of new pyrazole and isoxazole derivatives have been synthesised starting from pongamol a naturally occurring benzofuran derivative containing 1,3-diketone system. All the compounds have been characterised by their analytical and spectral data and were screened for their antifeedant activity,

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