In this study, 7 new isoxazole compounds () were synthesized from the cyclization of chalcone compounds () containing different functional groups with hydroxylamine hydrochloride in alkaline medium. Tyrosinase and antioxidant properties of were investigated. IC values for the tyrosinase enzyme inhibition of compounds , , , and were varied between 61.47 ± 3.46 and 188.52 ± 5.85, while compounds , and did not show any inhibition effect. The antioxidant properties of were investigated by DPPH and CUPRAC methods. Compound showed the best DPPH radical scavenging activity (SC: 40.21 ± 2.71), while and had shown the greatest Cupric ion reducing effect as 1.233 ± 0.015 and 1.245 ± 0.019 mg TEAC/mg, respectively. As a result, the change of functional groups in the synthesized compounds caused a significant difference in the biological properties of .
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http://dx.doi.org/10.55730/1300-0527.3364 | DOI Listing |
Int J Mol Sci
December 2024
Department of Organic Chemistry and Drug Technology, Faculty of Pharmacy, Wroclaw Medical University, 50-556 Wroclaw, Poland.
Microbiological communities have a significant impact on health and disease. are ubiquitous fungal pathogens that colonize the mucosal surfaces of the genital, urinary, respiratory, and gastrointestinal tracts, as well as the oral cavity. If the immune system is inadequate, then infections may pose a significant threat.
View Article and Find Full Text PDFChemMedChem
December 2024
Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Address 1Balanagar, Hyderabad, 500037, Telangana, India.
The continued prevalence of drug-resistant Mycobacterium tuberculosis (Mtb) strains, particularly against first-line antitubercular (anti-TB) drugs, presents an impending public health threat that necessitates the exploration and development of New Chemical Entities (NCEs). In search of new anti-TB leads, a library of ethyl 5-(1-benzyl-1H-indol-5-yl) isoxazole-3-carboxylates were generated through a strategy of scaffold hopping from the proven isoxazole-3-carboxylate-based anti-TB pharmacophore. We evaluated their antibacterial potential against a panel of pathogenic bacteria and Mtb HRv strains.
View Article and Find Full Text PDFBioorg Chem
January 2025
CSIR- Indian Institute of Integrative Medicine, Canal Road, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:
Alantolactone and isoalantolactone are two isomeric sesquiterpene lactones that were isolated from Innula recemosa. Here, we are used for the semisynthesis of novel isoxazolidine hybrids of alantolactone and isoalantolactone through a two-step process: nitrone synthesis followed by nitrone 1,3-dipolar cycloaddition. The formation of the cycloadduct was well characterized via modern spectroscopic techniques such as HRMS, H NMR, C NMR, DEPT-90, DEPT-135, and 2D NMR.
View Article and Find Full Text PDFACS Chem Neurosci
January 2025
Department of Anesthesiology and Perioperative Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, United States.
Co-use of xylazine with opioids is a major health threat in the United States. However, a critical knowledge gap exists in the understanding of xylazine-induced pharmacological and pathological impact. Xylazine is mostly known as an agonist of α2-adrenergic receptors (α2-ARs), but its deleterious effects on humans cannot be fully reversed by the α2-AR antagonists, suggesting the possibility that xylazine targets receptors other than α2-ARs.
View Article and Find Full Text PDFHeliyon
December 2024
Department of Biology, College of Science, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia.
The goal of this work was to synthesize new compounds for anticancer evaluation as a trial to obtain new antitumor agents with higher activity and fewer side effects. Therefore, the precursor 2,2'-(1,4-phenylenebis (thiazole-4,2-diyl))bis (3-(dimethylamino)acrylonitrile) was used to synthesize various azolopyrimidine derivatives connected to the thiazole moiety. Compounds -, including pyrazolopyrimidine, triazolopyrimidine, and others, were produced by reacting enaminonitrile with different -nucleophiles.
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