Isoxazole compounds exhibit a wide spectrum of targets and broad biological activities. Developing compounds with heterocycle rings has been one of the trends. The integration of isoxazole ring can offer improved physical-chemical properties. Because of the unique profiles, isoxazole ring becomes a popular moiety in compounds design. In this review article, the major focus has been paid to the applications of isoxazole compounds in treating multiple diseases, including anticancer, antimicrobial, anti-inflammatory, etc. Strategies for compounds design for preclinical, clinical, and FDA approved drugs were discussed. Also, the emphasis has been addressed to the future perspectives and trend for the application.
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http://dx.doi.org/10.1016/j.bmc.2018.05.013 | DOI Listing |
Med Chem
January 2025
Department of Pharmacy, Federal University of Sergipe, São Cristóvão, SE, Brazil.
Background: Owing to their extensive utilization as pesticides, heterocycles assume a fundamental role in the management of vector-borne diseases. Despite the presence of numerous heterocyclic compounds in commercial insecticides and larvicides, resistance to pesticides still demands novel strategies to current pest control methods. Considering these facts, this review aims to survey the synthesis and SAR of heterocyclic molecules with larvicidal activity against Aedes aegypti Linn.
View Article and Find Full Text PDFInt 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.
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