Beilstein Arch. 2022, 202231. https://doi.org/10.3762/bxiv.2022.31.v1
Published 29 Apr 2022
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.
|Format: DOC||Size: 86.0 KB||Download|
When a peer-reviewed version of this preprint is available, this information will be updated in the information box above. If no peer-reviewed version is available, please cite this preprint using the following information:
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
|Download RIS (Reference Manager)||Download BIB (BIBTEX)|
© 2022 da Silva et al.; licensee Beilstein-Institut.
This is an open access work licensed under the terms of the Beilstein-Institut Open Access License Agreement (https://www.beilstein-archives.org/xiv/terms), which is identical to the Creative Commons Attribution 4.0 International License (https://creativecommons.org/licenses/by/4.0). The reuse of material under this license requires that the author(s), source and license are credited. Third-party material in this work could be subject to other licenses (typically indicated in the credit line), and in this case, users are required to obtain permission from the license holder to reuse the material.