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Journal articles on the topic 'Oxazole derivative'

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Published: 4 June 2025

Last updated: 1 August 2025

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1

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-inflammato

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2

Kotha, Sambasivarao, and Subba Rao Cheekatla. "Synthesis of Bisoxazole and Bromo-substituted Aryloxazoles." Molbank 2022, no. 3 (2022): M1440. http://dx.doi.org/10.3390/m1440.

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Herein, we report a bisoxazole derivative as well as a bromo-substituted oxazole derivatives via a simple approach. The synthesis begins with an inexpensive and readily available starting material, such as 2,5-dimethoxybenzaldehyde, hydroquinone, and p-toluenesulfonylmethyl isocyanide (TosMIC). This approach relies on the Van Leusen oxazole method and electrophilic aromatic bromination. The structures of bisoxazole and bromosubstituted aryloxazoles were fully supported by spectroscopic methods (IR, NMR, and HRMS) and further established using single crystal X-ray diffraction studies.

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3

Kateryna, Matskevych. "Research of 1,3-oxazole-4-il-phosphonic acid derivative on the content of fatty acids of lipids in rats with arterial hypertension." ScienceRise: Pharmaceutical Science, no. 4(14) (August 31, 2018): 28–31. https://doi.org/10.15587/2519-4852.2018.141411.

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The number of patients with arterial hypertension (AH) continues to increase. Significant negative effects of arterial hypertension are structural, metabolic and functional disorders in the tissues of the myocardium, vessels and other organs, in particular, changes in the content of fatty acids (FA) and their correlation. The purpose of the study is to investigate the change in fatty acid composition of lipids in blood serum and tissues of rats with arterial hypertension under the influence of a new original compound, 1,3-oxazole-4-yl-phosphonic acid derivative (abbreviated name - oxazole deri

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4

Mistry, Rakesh N., and K. R. Desai. "Studies on Synthesis of Some Novel Heterocyclic Azlactone Derivatives and Imidazolinone Derivatives and their Antimicrobial Activity." E-Journal of Chemistry 2, no. 1 (2005): 42–51. http://dx.doi.org/10.1155/2005/542938.

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p- Methyl benzoic acid on reaction with phosphorus pentachloride gives p - methyl benzoyl chloride derivative which on condensation with glycine gives p - methyl benzoyl glycine derivative. Now, this p - methyl benzoyl glycine derivative on condensation with various substituted aldehydes gives corresponding substituted 4 - [aryl methylidine] - 2 - [p - methyl phenyl] - oxazole - 5 - one derivatives [1(a-j)]. Further, these derivatives [1(a-j)] on condensation with 4 , 4’ - diamino diphenyl sulphone gives corresponding substituted imidazolinone - dibenzsulphone derivatives [2(a-j)], on condensa

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5

Šagud, Ivana, Simona Božić, Željko Marinić, and Marija Šindler-Kulyk. "Photochemical approach to functionalized benzobicyclo[3.2.1]octene structures via fused oxazoline derivatives from 4- and 5-(o-vinylstyryl)oxazoles." Beilstein Journal of Organic Chemistry 10 (September 18, 2014): 2222–29. http://dx.doi.org/10.3762/bjoc.10.230.

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Novel cis/trans-4- and cis/trans-5-(2-vinylstyryl)oxazoles have been synthesized by Wittig reactions from the diphosphonium salt of α,α’-o-xylene dibromide, formaldehyde and 4- and 5-oxazolecarbaldehydes, respectively. In contrast, trans-5-(2-vinylstyryl)oxazole has been synthesized by the van Leusen reaction from trans-3-(2-vinylphenyl)acrylaldehyde which is prepared from o-vinylbenzaldehyde and (formylmethylene)triphenylphosphorane. The 4- and 5-(2-vinylstyryl)oxazoles afford, by photochemical intramolecular cycloaddition, diverse fused oxazoline-benzobicyclo[3.2.1]octadienes, which are iden

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6

Kenari, Marziyeh E., Joshua I. Putman, Ravi P. Singh, et al. "Enantiomeric Separation of New Chiral Azole Compounds." Molecules 26, no. 1 (2021): 213. http://dx.doi.org/10.3390/molecules26010213.

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Twelve new azole compounds were synthesized through an ene reaction involving methylidene heterocycles and phenylmaleimide, producing four oxazoles, five thiazoles, and one pyridine derivative, and ethyl glyoxylate for an oxazole and a thiazole compound. The twelve azoles have a stereogenic center in their structure. Hence, a method to separate the enantiomeric pairs, must be provided if any further study of chemical and pharmacological importance of these compounds is to be accomplished. Six chiral stationary phases were assayed: four were based on macrocyclic glycopeptide selectors and two o

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7

Stockert, Juan C. "Notes: Fluorescence of Chromatin DNA by an Oxazolium Scintillator." Zeitschrift für Naturforschung C 47, no. 5-6 (1992): 481–82. http://dx.doi.org/10.1515/znc-1992-0625.

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Aqueous solutions of a yellow and highly fluorescent derivative from dimethyl-POPOP, obtained by treating a chloroform solution of this oxazole scintillator with dimethylsulfate, induce a strong blue-green or yellowgreen fluorescence in chromatin DNA under ultraviolet (365 nm) or violet-blue (436 nm) excitation, respectively. It is suggested that this new and selective fluorescence reaction could originate from binding of the oxazolium derivative into the minor groove of DNA.

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8

Mcguire, Edward J., Robert H. Gray, and Felix A. De La Iglesia. "Chemical Structure-Activity Relationships: Peroxisome Proliferation and Lipid Regulation in Rats." Journal of the American College of Toxicology 11, no. 3 (1992): 353–61. http://dx.doi.org/10.3109/10915819209141875.

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Studies described here address structure-activity relationships of novel hypolipidemic agents that induce peroxisome proliferation. Male rats were given equivalent doses of three well-studied fibrates, fibrate amides, and structurally dissimilar agents. Aryloxyalkanoic acids, amide analogs, and thio, benzimidazole, phenylpiperazine, and oxazole derivatives induced peroxisome proliferation and decreased plasma cholesterol and triglyceride levels. These compounds contain an acidic function or appear to be readily metabolized to a derivative with an acidic function. Substitution of this substitue

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9

Venkatasubramanian H, Sarojkumar Sha, Hemalatha S, and Easwaramoorthy D. "Synthesis, characterization of new nicotinamide-oxazole analogs, and their antimicrobial activity." International Journal of Research in Pharmaceutical Sciences 11, no. 2 (2020): 2707–12. http://dx.doi.org/10.26452/ijrps.v11i2.2292.

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Identification of a novel antimicrobial molecule is vital to research due to contaminated agro related products and injurious pathogens. Especially candida albicans is most common infective fungi in the present world, that cause hospital-acquired infections. There is a medical and biological need for the discovery of novel antimicrobial drugs with high potent in nature. This effort involved the synthesis of scaffold molecule, in which Vitamin B3 and oxazole plays vital role as pharmacophore moiety, where 2-(Nicotinamido) oxazole-4-Carboxylic acid coupled from pyridine–3-carboxylic acid (Nicoti

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10

Heo, Yeongjae, Hyukmin Kwon, Sangwook Park, et al. "A High-Efficiency Deep Blue Emitter for OLEDs with a New Dual-Core Structure Incorporating ETL Characteristics." Molecules 28, no. 22 (2023): 7485. http://dx.doi.org/10.3390/molecules28227485.

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In this study, we introduced the weak electron-accepting oxazole derivative 4,5-diphenyl-2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)oxazole (TPO) into both anthracene and pyrene moieties of a dual core structure. Ultimately, we developed 2-(4-(6-(anthracen-9-yl)pyren-1-yl)phenyl)-4,5-diphenyloxazole (AP-TPO) as the substitution on the second core, pyrene, and 4,5-diphenyl-2-(4-(10-(pyren-1-yl)anthracen-9-yl)phenyl)oxazole (TPO-AP) as the substitution on the first core, anthracene. Both materials exhibited maximum photoluminescence wavelengths at 433 and 443 nm in solution and emi

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11

Lhoták, Pavel, and Antonín Kurfürst. "Synthesis of Luminophoric Derivatives of PBD Based on 2,5-Diaryl Substituted Thiazoles and Oxazoles." Collection of Czechoslovak Chemical Communications 58, no. 11 (1993): 2720–28. http://dx.doi.org/10.1135/cccc19932720.

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The Friedel-Crafts acylation of 2-(biphenyl-4-yl)-5-phenyl-1,3,4-oxadiazole (PBD) with hippuryl chloride has been used to prepare the derivative V which on cyclization with POCl3 or P4S10 gives the respective oxazole (or thiazole) derivative of PBD, XIa or XIb. The reaction of carboxylic acid II with 4-(o-aminoacetyl)biphenyl in the presence of CDI gives N-acyl-α-aminoketone VII; the analogous compound VI has been prepared by acylating of o-aminoacetophenone with acyl chloride III. The cyclization of these compounds gives bifluorophores Xa - Xd.

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12

A.H. Abdullah, Sallal, and Jaafar Sataar Shia. "Synthesis of some metal ion complexes of new imidazole derivative, characterization, and biological activity." Bulletin of the Chemical Society of Ethiopia 38, no. 6 (2024): 1681–90. http://dx.doi.org/10.4314/bcse.v38i6.14.

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Imidazole complexes with high biological activity for some metal complexes prepared by a new imidazole ligand from the reaction of a 1,3-oxazole derivative with hydroxylamine and utilizing this ligand in the preparation of some metal ion complexes. Many of the techniques available for all prepared compounds, such as elemental analysis (CHNS), (FT-IR), (UV-Vis) spectra, and 1H-NMR spectra, will be used in the diagnosis of these complexes, and the forms of the complexes will be deduced from the results obtained. The outcomes demonstrated that the octahedral geometries of all the produced complex

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13

Shibata, Katsunori, Lumi Kuroki, Tuyoshi Fukaminato, and Masahiro Irie. "Fluorescence Switching of a Diarylethene Derivative Having Oxazole Rings." Chemistry Letters 37, no. 8 (2008): 832–33. http://dx.doi.org/10.1246/cl.2008.832.

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14

Apostol, Theodora-Venera, Mariana Carmen Chifiriuc, George Mihai Nitulescu, et al. "In Silico and In Vitro Assessment of Antimicrobial and Antibiofilm Activity of Some 1,3-Oxazole-Based Compounds and Their Isosteric Analogues." Applied Sciences 12, no. 11 (2022): 5571. http://dx.doi.org/10.3390/app12115571.

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In this paper, we report on the antimicrobial activity assessment of 49 compounds previously synthesized as derivatives of alanine or phenylalanine that incorporate a 4-(4-X-phenylsulfonyl)phenyl fragment (X = H, Cl, or Br), namely 21 acyclic compounds (6 × N-acyl-α-amino acids, 1 × N-acyl-α-amino acid ester, and 14 × N-acyl-α-amino ketones) and 28 pentatomic heterocycles from the oxazole-based compound class (6 × 4H-1,3-oxazol-5-ones, 16 × 5-aryl-1,3-oxazoles, and 6 × ethyl 1,3-oxazol-5-yl carbonates). Both in silico and in vitro qualitative and quantitative assays were used to investigate th

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15

Phalke, Pallavi L. "Synthesis of different α, β- unsaturated oxazolone derivatives". Journal of Drug Delivery and Therapeutics 9, № 1 (2019): 124–27. http://dx.doi.org/10.22270/jddt.v9i1.2189.

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Acetyl glycine were prepared from glycine acetic anhydride and then 2, 4-disubstituted Oxazol-5-one were prepared from acetyl glycine, substituted aldehydes, acetic anhydride, and sodium acetate as a catalyst. The formed product is evaluated and characterized by thin layer chromatography, infrared spectroscopy and melting point. The, β- unsaturated shows ability to react with various nucleophilic reagents for synthesis of new fused oxazole compounds. Keywords: glycine, acetic anhydride, aldehyde Sodium acetate, Oxazolone, E. coli, Antibacterial Activity.

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16

Mavridis, Evangelos, Eleftherios Bermperoglou, Eleni Pontiki, and Dimitra Hadjipavlou-Litina. "5-(4H)-Oxazolones and Their Benzamides as Potential Bioactive Small Molecules." Molecules 25, no. 14 (2020): 3173. http://dx.doi.org/10.3390/molecules25143173.

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The five membered heterocyclic oxazole group plays an important role in drug discovery. Oxazolones present a wide range of biological activities. In this article the synthesis of 4-substituted-2-phenyloxazol-5(4H)-ones from the appropriate substituted aldehydes via an Erlenmeyer–Plochl reaction is reported. Subsequently, the corresponding benzamides were produced via a nucleophilic attack of a secondary amine on the oxazolone ring applying microwave irradiation. The compounds are obtained in good yields up to 94% and their structures were confirmed using IR, 1H-NMR, 13C-NMR and LC/MS data. The

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17

Pu, Xiang, Guangzhou Li, Tao Yang, et al. "A new cyclododeca[d]oxazole derivative from Streptomyces spp. CIBYL1." Natural Product Research 27, no. 7 (2012): 603–8. http://dx.doi.org/10.1080/14786419.2012.682997.

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18

Khokhlov, Alexander L., Ilya I. Yaichkov, Anton А. Shetnev, et al. "Identification and synthesis of metabolites of the new antiglaucoma drug." Research Results in Pharmacology 10, no. 1 (2023): 53–66. http://dx.doi.org/10.18413/rrpharmacology.10.431.

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Introduction: The determination of biotransformation products is an essential part of the preclinical trial of original medicines. These studies have not been conducted before for the new drug 5-[5-(trifluoromethyl)-1,2-oxazole-3-yl]-furan-2-sulfonamide. Identification and synthesis of metabolite substances are necessary for subsequent tests of bioavailability, linearity of pharmacokinetics, accumulation, distribution and excretion. Materials and methods: The study was carried out on Wistar rats and rabbits of the Soviet Chinchilla breed. The substance of the drug was administered to animals i

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19

He, Yuan, Ting Zheng, Yin-Hui Huang, and Lin Dong. "Rh(iii)-Catalyzed olefination to build diverse oxazole derivatives from functional alkynes." Organic & Biomolecular Chemistry 19, no. 22 (2021): 4937–42. http://dx.doi.org/10.1039/d1ob00507c.

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20

Gangloff, Anthony R., Bjoern Aakermark, and Paul Helquist. "Generation and use of a zinc derivative of a functionalized 1,3-oxazole. Solution of the virginiamycin/madumycin oxazole problem." Journal of Organic Chemistry 57, no. 18 (1992): 4797–99. http://dx.doi.org/10.1021/jo00044a009.

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21

Shinozaki, Yoshinao, Isao Yoshikawa, Koji Araki, et al. "Coordination Oligomers and Polymers of an Oxazole-appended Zinc Chlorophyll Derivative." Chemistry Letters 43, no. 6 (2014): 862–64. http://dx.doi.org/10.1246/cl.140135.

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22

Khokhlov, Alexander L., Ilya I. Yaichkov, Mikhail A. Alexeev, et al. "Identification and synthesis of metabolites of the new 4.5-dihydroisoxazol-5-carboxamide derivate." Research Results in Pharmacology 10, no. 2 (2024): 83–95. http://dx.doi.org/10.18413/rrpharmacology.10.482.

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Introduction: 3-(2-butyl-5-chloro-1H-imidazole-4-yl)-N-[4-methoxy-3-(trifluoromethyl)phenyl]-4,5-dihydro-1,2-oxazole-5-carboxamide is new antirheumatic drug. It is necessary to identify and synthesize the biotransformation products for its complete pharmacokinetic study. Materials and Methods: A biotransformation study was carried out by intraperitoneal administration of the drug to Wistar rats and Soviet Chinchilla breed rabbits. Animal blood sampling was performed before the injection and 0.5 h, 1 h, 2 h, 4 h, 24 h after the injection of the investigated compound. The samples were immediatel

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23

Apostol, Theodora-Venera, Mariana Carmen Chifiriuc, Constantin Draghici, et al. "Synthesis, In Silico and In Vitro Evaluation of Antimicrobial and Toxicity Features of New 4-[(4-Chlorophenyl)sulfonyl]benzoic Acid Derivatives." Molecules 26, no. 16 (2021): 5107. http://dx.doi.org/10.3390/molecules26165107.

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The multi-step synthesis, physico-chemical characterization, and biological activity of novel valine-derived compounds, i.e., N-acyl-α-amino acids, 1,3-oxazol-5(4H)-ones, N-acyl-α-amino ketones, and 1,3-oxazoles derivatives, bearing a 4-[(4-chlorophenyl)sulfonyl]phenyl moiety are reported here. The structures of the newly synthesized compounds were confirmed by spectral (UV-Vis, FT-IR, MS, 1H- and 13C-NMR) data and elemental analysis results, and their purity was determined by RP-HPLC. The new compounds were assessed for their antimicrobial activity and toxicity to aquatic crustacean Daphnia m

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24

GANGLOFF, A. R., B. AKERMARK, and P. HELQUIST. "ChemInform Abstract: Generation and Use of a Zinc Derivative of a Functionalized 1,3- Oxazole. Solution of the Virginiamycin/Madumycin Oxazole Problem." ChemInform 24, no. 5 (2010): no. http://dx.doi.org/10.1002/chin.199305177.

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25

Kuna, Krishna Vadiyala Naveen Reddy and Tigulla Parthasarathy *. "SYNTHESIS, BIOLOGICAL EVALUATION AND MODELING STUDIES OF 2-(4-((1H-1,2,3-TRIAZOL-4-YL)METHOXY)PHENYL)BENZO[D]OXAZOLE AND 2-(4-((2-ALKYL-2H-TETRAZOL-5-YL)METHOXY)PHENYL) BENZO[D]OXAZOLES AS A NOVEL ANTIMICROBIAL AGENTS." Journal of Pharma Research 6, no. 12 (2017): 208–14. https://doi.org/10.5281/zenodo.1129468.

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<strong><em>ABSTRACT</em></strong> <strong><em>A</em></strong><em> series of triazole <strong>(6a-f)</strong> and tetrazole <strong>(7a-f)</strong> derivatives were synthesized and </em><em>their structures were confirmed by IR, 1HNMR and mass spectroscopic studies.</em><em> All the compounds have been screened for their antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli and antifungal activity against Aspergillus fumigates Aspergillus niger and Candida albicans. Evaluation of antimicrobial activity considering the MIC value calculated by the seri

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26

Mai, A., M. Artico, G. Sbardella, et al. "Arylketotetramethylene Analogues of Disoxaril with Anti-Human Rhinovirus 14 Activity." Antiviral Chemistry and Chemotherapy 8, no. 3 (1997): 235–42. http://dx.doi.org/10.1177/095632029700800307.

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Arylketotetramethylene analogues of disoxaril (WIN 51711) were synthesized by reaction of 1-aryl-5-chloropentan-1-ones with 2-(4-hydroxyphenyl)-4,5-dihydro oxazoles, ethyl 4-hydroxybenzoates and 4-hydroxybenzonitrile. The new derivatives were tested for antiviral activity against various human rhinovirus (HRV) serotypes. The best activity was exhibited by the ethoxycarbonyl derivatives, whereas the oxazoline counterparts were less active and the cyano derivatives totally inactive. 5-[4-(4,5-Dihydro-2-oxazolyl)phenoxy]-1-(4-methoxyphenyl)pentan-1-one and ethyl 4-[5-(4-methylthiophenyl)-5-oxopen

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27

Yaichkov, I. I., A. L. Khokhlov, M. K. Korsakov, A. A. Shetnev, N. N. Volkhin, and S. S. Petukhov. "Pharmacokinetics Study of a New Isoxazole Derivative in Rats Using HPLC-MS/MS for Blood Sample Analysis." Regulatory Research and Medicine Evaluation 14, no. 3 (2024): 304–16. http://dx.doi.org/10.30895/1991-2919-2024-14-3-304-316.

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INTRODUCTION. Systemic exposure studies of a selective carbonic anhydrase II inhibitor, the isoxazole derivative 5-[5-(trifluoromethyl)-1,2-oxazole-3-yl]-furan-2-sulfonamide (TFISA), require evaluating its pharmacokinetics in whole blood because the compound can accumulate in erythrocytes. Currently, no bioanalytical procedures have been developed to achieve this.AIM. This study aimed to develop a bioanalytical procedure for the determination of TFISA and its metabolites (N-hydroxy-5-[5-(trifluoromethyl)-1,2-oxazole-3-yl]-furan-2-sulfonamide and N-acetyl-5-[5-(trifluoromethyl)-1,2-oxazole-3-yl

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28

Mori, Yukie, and Koko Maeda. "Novel photochemical rearrangement of 2,4,4,6-tetraphenylpyridin-3(4H)-one to an oxazole derivative." Journal of the Chemical Society, Chemical Communications, no. 17 (1991): 1200. http://dx.doi.org/10.1039/c39910001200.

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29

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

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Reactions of indole-2,3-dione 1 with 2-mercaptobenzimidazole, o-phenylenediamine, 2-aminophenol, 2-aminobenzothiazole, 2-aminobenzimidazole and 3-methyl-1-phenyl-2-pyrazolin-5-one were carried out to give compounds spiroindolethiazetobenzimidazole 2, spirobenzimidazole(oxazole)indoline 3a,b, benzothiazol(imidazol) iminoindolinone 4a,b and methyloxoindolylidenepyrazolone 5 respectively. Compound 5 was reacted with 2-aminophenol as well as o-phenylenediamine to give new spirooxazepine and diazepine derivatives 6a,b respectively. Reaction of 5 with nitrogen nucleophiles as well as carbon nucleoph

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30

Tsygankova, V.A., Ya.V. Andrusevich, O.I. Shtompel, S.G. Pilyo, A.M. Kornienko, and V.S. Brovarets. "Using of [1,3]oxazolo[5,4-d]pyrimidine and N-sulfonyl substituted of 1,3-oxazole to improve the growth of soybean seedlings." Chemistry Research Journal 3, no. 2 (2018): 165–73. https://doi.org/10.5281/zenodo.13923631.

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The effect of the chemical low molecular weight heterocyclic compounds, derivatives of [1,3]oxazolo[5,4-<em>d</em>]pyrimidine and N-sulfonylsubstituted of 1,3-oxazole on stimulation of root and shoot growth of soybean seedlings (<em>Glycine max </em>L.) cultivar Valuta was studied. The growth regulating activity of the heterocyclic compounds derivatives of [1,3]oxazolo[5,4-<em>d</em>]pyrimidine and N-sulfonyl substituted of 1,3-oxazole was compared with the growth regulating activity of the plant hormone auxin NAA (1-Naphthylacetic acid). It was found that the chemical heterocyclic compounds u

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31

Alkhaldi, Abdulsalam A. M., Mohamed A. Abdelgawad, Bahaa G. M. Youssif, Ahmed O. El-Gendy, and Harry P. De Koning. "Synthesis, antimicrobial activities and GAPDH docking of novel 1, 2, 3-triazole derivatives." Tropical Journal of Pharmaceutical Research 18, no. 5 (2021): 1101–8. http://dx.doi.org/10.4314/tjpr.v18i5.27.

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Purpose: To synthesize new triazole derivatives in order to overcome the problem of side effects of antimicrobial agents and microbial resistance, while broadening the spectrum of antimicrobial activity. Methods: The starting triazole, compound 1, was prepared through click chemistry and reacted with chloroacetyl chloride to yield compound II. Triazole 1 was reacted with acids and aldehydes to produce oxadiazole (III) and azomethine (IV) which cyclized in acetic anhydride to give a new acetylated oxadiazole (V). Minimum inhibitory concentration (MIC) and resorufin assays were used for an

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32

Belaidi, Salah, and Malika Mellaoui. "Electronic Structure and Physical-Chemistry Property Relationship for Oxazole Derivatives by Ab Initio and DFT Methods." Organic Chemistry International 2011 (September 12, 2011): 1–7. http://dx.doi.org/10.1155/2011/254064.

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The geometric, electronic structure, effect of the substitution, and structure physical-chemistry relationship for oxazoles derivatives have been studied by ab initio and DFT theory. In the present work, the calculated values, namely, net charges, bond lengths, dipole moments, electron affinities, heats of formation, and QSAR properties are reported and discussed in terms of the reactivity of oxazole derivatives.

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33

Khokhlov, A. L., I. I. Yaichkov, A. A. Shetnev, et al. "Study of biotransformation of new selective carbonic anhydrase II inhibitor 4-(2-methyl-1,3-oxazole-5-yl)-benzenesulfonamide." Pharmacy & Pharmacology 11, no. 3 (2023): 240–54. http://dx.doi.org/10.19163/2307-9266-2023-11-3-240-254.

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The aim of the study was to determine biotransformation products of a new selective carbonic anhydrase II inhibitor – 4-(2-methyl-1,3-oxazole-5-yl)-benzenesulfonamide.Materials and methods. The study was conducted on 3 Wistar rats and 3 rabbits of the Soviet Chinchilla breed. The suspension of the drug was administered intraperitoneally to rats at a dosage of 20 mg/kg, to rabbits - at a dosage of 1.6 mg/kg. The animal blood samples were collected before the administration and 1, 2, 4, 24 h after. Urine sampling was also performed in the rats before the administration and in the intervals of 0–

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Song, Yin-Ping, Feng-Ping Miao, Sheng-Tao Fang, Xiu-Li Yin, and Nai-Yun Ji. "Halogenated and Nonhalogenated Metabolites from the Marine-Alga-Endophytic Fungus Trichoderma asperellum cf44-2." Marine Drugs 16, no. 8 (2018): 266. http://dx.doi.org/10.3390/md16080266.

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One new bisabolane sesquiterpene, bisabolan-1,10,11-triol (1), one new norbisabolane sesquiterpene, 12-nor-11-acetoxybisabolen-3,6,7-triol (2), two new naturally occurring monoterpenes, (7S)- and (7R)-1-hydroxy-3-p-menthen-9-oic acids (3 and 4), one new naturally occurring trichodenone, dechlorotrichodenone C (5), one new chlorine-containing trichodenone, 3-hydroxytrichodenone C (6), one new diketopiperazine, methylcordysinin A (7), and one new naturally occurring oxazole derivative, 4-oxazolepropanoic acid (8), were isolated from the culture of a marine brown alga-endophytic strain (cf44-2) o

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Chiacchio, Maria A., Giuseppe Lanza, Ugo Chiacchio, et al. "Oxazole-Based Compounds As Anticancer Agents." Current Medicinal Chemistry 26, no. 41 (2020): 7337–71. http://dx.doi.org/10.2174/0929867326666181203130402.

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: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivative

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Linder, Jörg, Alexander J. Blake, and Christopher J. Moody. "Total synthesis of siphonazole and its O-methyl derivative, structurally unusual bis-oxazole natural products." Organic & Biomolecular Chemistry 6, no. 21 (2008): 3908. http://dx.doi.org/10.1039/b810855b.

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Chen, Lulu, Zhi Ren, Xuedong Zhou, Jumei Zeng, Jing Zou, and Yuqing Li. "Inhibition of Streptococcus mutans biofilm formation, extracellular polysaccharide production, and virulence by an oxazole derivative." Applied Microbiology and Biotechnology 100, no. 2 (2015): 857–67. http://dx.doi.org/10.1007/s00253-015-7092-1.

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MORI, Y., and K. MAEDA. "ChemInform Abstract: Novel Photochemical Rearrangement of 2,4,4,6-Tetraphenylpyridin-3(4H)- one to an Oxazole Derivative." ChemInform 23, no. 12 (2010): no. http://dx.doi.org/10.1002/chin.199212083.

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Nizhenkovska, I. V., V. K. Sedko, O. V. Golovchenko, and O. I. Golovchenko. "The study of acute toxicity of 1,3-oxazole-4-il-phosphonic acid derivative in intraperitoneal administration." Vìsnik farmacìï, no. 1(93) (March 15, 2018): 43–48. http://dx.doi.org/10.24959/nphj.18.2186.

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Teder, Tarvi, Stefanie König, Rajkumar Singh, et al. "Modulation of the 5-Lipoxygenase Pathway by Chalcogen-Containing Inhibitors of Leukotriene A4 Hydrolase." International Journal of Molecular Sciences 24, no. 8 (2023): 7539. http://dx.doi.org/10.3390/ijms24087539.

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The 5-lipoxygenase (5-LOX) pathway gives rise to bioactive inflammatory lipid mediators, such as leukotrienes (LTs). 5-LOX carries out the oxygenation of arachidonic acid to the 5-hydroperoxy derivative and then to the leukotriene A4 epoxide which is converted to a chemotactic leukotriene B4 (LTB4) by leukotriene A4 hydrolase (LTA4H). In addition, LTA4H possesses aminopeptidase activity to cleave the N-terminal proline of a pro-inflammatory tripeptide, prolyl-glycyl-proline (PGP). Based on the structural characteristics of LTA4H, it is possible to selectively inhibit the epoxide hydrolase acti

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Irfan, Ahmad, Abdullah G. Al-Sehemi, Aijaz Rasool Chaudhry, and Shabbir Muhammad. "The structural, electro-optical, charge transport and nonlinear optical properties of oxazole (4 Z )-4-Benzylidene-2-(4-methylphenyl)-1,3-oxazol-5(4 H )-one derivative." Journal of King Saud University - Science 30, no. 1 (2018): 75–82. http://dx.doi.org/10.1016/j.jksus.2016.10.004.

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Kubicki, Maciej, Agata Owczarzak, Anita M. Grzeskiewicz, Tomasz Stefanski, and Zbigniew Dutkiewicz. "The halogen C—Br...S bonding in the crystal structure of an oxazole derivative: a charge-density study." Acta Crystallographica Section A Foundations and Advances 74, a2 (2018): e336-e336. http://dx.doi.org/10.1107/s2053273318090150.

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NESI, R., S. TURCHI, and D. GIOMI. "ChemInform Abstract: New Perspectives in Oxazole Chemistry: Synthesis and Cycloaddition Reactions of a 4-Nitro-2-phenyl Derivative." ChemInform 28, no. 10 (2010): no. http://dx.doi.org/10.1002/chin.199710111.

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Tsygankova, V.A., Ya.V. Andrusevich, O.I. Shtompel, A.M. Kornienko, V.S. Brovarets, and S.G. Pilyo. "Acceleration of vegetative growth of wheat (Triticum aestivum L.) using [1,3]oxazolo[5,4-d]pyrimidine and N-sulfonyl substituted 1,3-oxazole." Pharmaceutical and Chemical Journal 5, no. 2 (2018): 167–75. https://doi.org/10.5281/zenodo.13904610.

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Wheat (<em>Triticum aestivum</em> L.) is an important cereal crop cultivated in the most economically developed coutries. The elaboration of new effective growth regulators for intensification of seed germination stage and vegetative growth of wheat is an actual problem for modern agriculture. In our work the comparative analysis of regulating activity of low molecular weight heterocyclic compounds, derivatives of [1,3]oxazolo[5,4-<em>d</em>]pyrimidine and N-sulfonyl substituted of 1,3-oxazole, and plant hormones auxins IAA (1<em>H</em>-Indol-3-ylacetic acid) and NAA (1-Naphthylacetic acid) on

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Özil, Musa, and Emre Menteşe. "Microwave-assisted Synthesis of Benzoxazoles Derivatives." Current Microwave Chemistry 7, no. 3 (2020): 183–95. http://dx.doi.org/10.2174/2213335607999200518094114.

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Background: Benzoxazole, containing a 1,3-oxazole system fused with a benzene ring, has a profound effect on medicinal chemistry research owing to its important pharmacological activities. On the other hand, the benzoxazole derivative has exhibited important properties in material science. Especially in recent years, microwave-assisted synthesis is a technique that can be used to increase diversity and quick research in modern chemistry. The utilization of microwave irradiation is beneficial for the synthesis of benzoxazole in recent years. In this focused review, we provide a metaanalysis of

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Yang, Feihu, Xiaojie Zheng, Qiong Hu, Yimin Hu, Yu Lei, and Wenjing Zhu. "Epoxyanthracene Derivatives and Dicarbonylation on Benzene Ring via Hexadehydro-Diels–Alder (HDDA) Derived Benzynes with Oxazoles." Synthesis 54, no. 04 (2021): 1125–33. http://dx.doi.org/10.1055/a-1659-8167.

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AbstractA capture reaction of hexadehydro-Diels–Alder (HDDA) derived benzyne with various substituted oxazoles is reported. With methyl, hydrogen, or phenyl as the substituent at 2-position of oxazole, tetraynes afforded epoxyanthracene derivatives or underwent dicarbonylation on benzene ring. The reaction does not require any catalyst or additive. The mechanism behind the reaction was investigated. The obtained polycyclic product structure has potential application value in optoelectronic materials. The availability of dicarbonylated arene implies the uniqueness of HDDA benzyne reaction compa

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Brusnakov, Mykhailo, Oleksandr Golovchenko, Lyudmyla Potikha, and Volodymyr Brovarets. "1,3-Oxazoles as precursors of phosphorylated amino acids and peptidomimetics." Ukr. Bioorg. Acta 2022, Vol. 17, N1 17, no. 1 (2022): 72–80. http://dx.doi.org/10.15407/bioorganica2022.01.072.

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The design and development of new phosphorus-containing amino acids and peptidomimetics have been attracting considerable attention due to their value as intermediates in the synthesis of biologically active compounds and the prospects for further pharmacological applications. 1,3-Oxazole derivatives, as masked peptides, constitute an important group of amino acid precursors that are widely used in contemporary organic synthesis. This review presents the 1,3-oxazole-based synthetic strategies of phosphorylated amino acids and peptides that have been published in both journal and patent literat

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Nizhenkovska, Iryna, Kateryna Sedko, and Olena Kuznetsova. "Study of influence of 1,3-oxazole-4-yl-phosphonic acid derivative on nitric oxide system indicators in rats with arterial hypertension." Česká a slovenská farmacie 67, no. 4 (2018): 154–59. https://doi.org/10.36290/csf.2018.022.

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Li, Xiao, Xiao-Ting Yu, Hai-Jun Chi, et al. "Synthesis, photophysical, electrochemical and electroluminescent properties of a novel iridium(III) complex based on 2-phenylbenzo[d]oxazole derivative." Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 116 (December 2013): 473–77. http://dx.doi.org/10.1016/j.saa.2013.07.075.

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Bahrieieva, Oksana S., Oleksandr V. Golovchenko, Oksana I. Golovchenko, Victor V. Zhirnov, and Volodymyr S. Brovarets. "New phosphorylated 5-(hydroxyalkylamino)-1,3-oxazoles as potential anticancer agents." Ukr. Bioorg. Acta 2023, Vol. 18, N1 18, no. 1 (2023): 32–41. http://dx.doi.org/10.15407/bioorganica2023.01.032.

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Eight new phosphorylated 5-(hydroxyalkylamino)-1,3-oxazoles were designed and tested for their ability to inhibit cancer cell growth. These compounds were evaluated against complete human tumor cell lines NCI-60. Only three compounds showed antitumor activity in the single dose assay, which were taken in the five dose assay. Compounds 7 and 8 showed the same average antiproliferative activity and cytotoxicity against sensitive cell lines of the general panel. However, compound 8 showed cytotoxicity to more lines than 7. By all parameters, these compounds were more active than compounds 5. Comp

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