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Sustainable Development Goals
03 Saúde e Bem-EstarCollections
- IOC - Artigos de Periódicos [12968]
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IN SILICO AND PHARMACOLOGICAL STUDY OF N,S-ACETAL JUGLONE DERIVATIVES AS INHIBITORS OF THE P2X7 RECEPTOR-PROMOTED IN VITRO AND IN VIVO INFLAMMATORY RESPONSE
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Abstract
Purinergic receptors are transmembrane proteins responsive to extracellular nucleotides and are expressed by
several cell types throughout the human body. Among all identified subtypes, the P2×7 receptor has emerged as
a relevant target for the treatment of inflammatory disease. Several clinical trials have been conducted to
evaluate the effectiveness of P2×7R antagonists. However, to date, no selective antagonist has reached clinical
use. In this work, we report the pharmacological evaluation of eleven N, S-acetal juglone derivatives as P2×7R
inhibitors. Using in vitro assays and in vivo experimental models, we identified one derivative with promising
inhibitory activity and low toxicity. Our in silico studies indicate that the 1,4-naphthoquinone moiety might be a
valuable molecular scaffold for the development of novel P2×7R antagonists, as suggested by our previous
studies.
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