Evaluation of Thiazolidine Derivatives with Potential Anti-ZIKV Activity.

Autor:	Gonçalves SMC; Therapeutic Innovation Research Center, Federal University of Pernambuco, Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., Galdino LV; Therapeutic Innovation Research Center, Federal University of Pernambuco, Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., Lima MC; Department of Virology and Experimental Therapy, Aggeu Magalhães Institute, Oswaldo Cruz Foundation / FIOCRUZ, Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., da Silva Moura JA; Pharmaceutical Planning and Synthesis Laboratory, Federal University of Pernambuco Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., Viana DCF; Pharmaceutical Planning and Synthesis Laboratory, Federal University of Pernambuco Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., da Rosa MM; Therapeutic Innovation Research Center, Federal University of Pernambuco, Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., Ferreira LFGR; Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Artur de Sá, Recife-PE, 50740-521, Brazil., Hernandes MZ; Department of Pharmaceutical Sciences, Federal University of Pernambuco, Av. Prof. Artur de Sá, Recife-PE, 50740-521, Brazil., Pereira MC; Therapeutic Innovation Research Center, Federal University of Pernambuco, Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., de Melo Rêgo MJB; Therapeutic Innovation Research Center, Federal University of Pernambuco, Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., da Rocha Pitta I; Pharmaceutical Planning and Synthesis Laboratory, Federal University of Pernambuco Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., de Oliveira França R; Department of Virology and Experimental Therapy, Aggeu Magalhães Institute, Oswaldo Cruz Foundation / FIOCRUZ, Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., da Rocha Pitta MG; Pharmaceutical Planning and Synthesis Laboratory, Federal University of Pernambuco Av. Moraes Rego, 1235, Recife, 50670-901, Brazil., da Rocha Pitta MG; Therapeutic Innovation Research Center, Federal University of Pernambuco, Av. Moraes Rego, 1235, Recife, 50670-901, Brazil.
Jazyk:	angličtina
Zdroj:	Current topics in medicinal chemistry [Curr Top Med Chem] 2024; Vol. 24 (25), pp. 2224-2237.
DOI:	10.2174/0115680266315388240801053401
Abstrakt:	Objective: In this study, we have synthesized 19 Thiazolidine (TZD) derivatives to investigate their potential anti-ZIKV effects. Methods: Nineteen thiazolidine derivatives were synthesized and evaluated for their cytotoxicity and antiviral activity against the ZIKA virus. Results: Among them, six demonstrated remarkable selectivity against the ZIKV virus, exhibiting IC50 values of <5μM, and the other compounds did not demonstrate selectivity for the virus. Interestingly, several derivatives effectively suppressed the replication of ZIKV RNA copies, with derivatives significantly reducing ZIKV mRNA levels at 24 hours post-infection (hpi). Notably, two derivatives (ZKC-4 and -9) stood out by demonstrating a protective effect against ZIKV cell entry. Informed by computational analysis of binding affinity and intermolecular interactions within the NS5 domain's N-7 and O'2 positions, ZKC-4 and FT-39 displayed the highest predicted affinities. Intriguingly, ZKC-4 and ZKC-9 derivatives exhibited the most favorable predicted binding affinities for the ZIKV-E binding site. Conclusion: The significance of TZDs as potent antiviral agents is underscored by these findings, suggesting that exploring TZD derivatives holds promise for advancing antiviral therapeutic strategies. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
Databáze:	MEDLINE
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