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Serrano JL, Lopes D, Reis MJA, et al. Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation. Biomedicines. 2021;9(10)doi: 10.3390/biomedicines9101443.
Serrano, J. L., Lopes, D., Reis, M. J. A., Boto, R. E. F., Silvestre, S., & Almeida, P. (2021). Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation. Biomedicines, 9(10), . https://doi.org/10.3390/biomedicines9101443
Serrano, João L, et al. "Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation." Biomedicines vol. 9,10 (2021). doi: https://doi.org/10.3390/biomedicines9101443
Serrano JL, Lopes D, Reis MJA, Boto REF, Silvestre S, Almeida P. Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation. Biomedicines. 2021 Oct 11;9(10). doi: 10.3390/biomedicines9101443. PMID: 34680559; PMCID: PMC8533253.
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Biomedicines. 2021 Oct 11;9(10). doi: 10.3390/biomedicines9101443.

Bis-thiobarbiturates as Promising Xanthine Oxidase Inhibitors: Synthesis and Biological Evaluation.

Biomedicines

João L Serrano, Diana Lopes, Melani J A Reis, Renato E F Boto, Samuel Silvestre, Paulo Almeida

Affiliations

  1. CICS-UBI-Health Sciences Research Center, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal.
  2. CNC-Center for Neuroscience and Cell Biology, University of Coimbra, Rua Larga, 3004-517 Coimbra, Portugal.

PMID: 34680559 PMCID: PMC8533253 DOI: 10.3390/biomedicines9101443

Abstract

Xanthine oxidase (XO) is the enzyme responsible for the conversion of endogenous purines into uric acid. Therefore, this enzyme has been associated with pathological conditions caused by hyperuricemia, such as the disease commonly known as gout. Barbiturates and their congeners thiobarbiturates represent a class of heterocyclic drugs capable of influencing neurotransmission. However, in recent years a very large group of potential pharmaceutical and medicinal applications have been related to their structure. This great diversity of biological activities is directly linked to the enormous opportunities found for chemical change off the back of these findings. With this in mind, sixteen bis-thiobarbiturates were synthesized in moderate to excellent reactional yields, and their antioxidant, anti-proliferative, and XO inhibitory activity were evaluated. In general, all bis-thiobarbiturates present a good antioxidant performance and an excellent ability to inhibit XO at a concentration of 30 µM, eight of them are superior to those observed with the reference drug allopurinol (Allo), nevertheless they were not as effective as febuxostat. The most powerful bis-thiobarbiturate within this set showed in vitro IC

Keywords: antioxidant; bis-thiobarbiturates; cytotoxicity; in silico evaluation; xanthine oxidase

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