New triazole triterpene derivative exhibits anti-RSV activity synthesis biological evaluation and molecular modeling

Submitting author affiliation:
Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil

Beilstein Arch. 2022, 202231.

Published 29 Apr 2022

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Respiratory syncytial virus (RSV) is a major cause of acute lower respiratory tract infections in infants. Currently, ribavirin, a nucleoside analog containing 1,2,4-triazole-3-carboxamide moiety, is a first-line drug for its treatment, however, its clinical use has been limited due to its side effects. Here, we designed a new aryl-nitro-1,2,3-triazole triterpenes derivatives as novel anti-RSV drugs. Their anti-RSV and cytotoxic activity were evaluated in vitro, RSV protein F gene effects by RT-PCR and molecular modeling IMPDH enzyme was performed. Compound 8 was the best performing compound, with EC50 values of 0.053μM and a TI of 11160.37 and it inhibited hRSV protein F gene expression by approximately 65%. Molecular docking showed a top-ranked solution located in the same region occupied by crystallographic ligands in their complex with IMPDH. The results obtained in this study suggests that compound 8 might be a new anti- candidate.

Keywords: Antiviral, bioisosterism, respiratory syncytial virus, triterpene, betulinic acid, ursolic acid.

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da Silva, E. F.; Fernandes, K. H. A.; Diedrich, D.; Gotardi, J.; Franco, M. S. F.; da Silva, C. H. T. D. P.; de Souza, A. P. D.; Gnoatto, S. C. B. Beilstein Arch. 2022, 202231. doi:10.3762/bxiv.2022.31.v1

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