New triazole-substituted triterpene derivatives exhibiting anti-RSV activity: synthesis, biological evaluation, and molecular modeling

Silva, Elenilson Figueiredo da; Antunes, Krist Helen; Diedrich, Denise; Gotardi, Jessica; Franco, Márcia Silvana Freire; Silva, Carlos Henrique Tomich de Paula da; Souza, Ana Paula Duarte de; Gnoatto, Simone Cristina Baggio

doi:10.3762/bjoc.18.161

Cited by 5 publications

(7 citation statements)

References 38 publications

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“…Cost-effectiveness analyses are crucial for regional and global healthcare policy-makers, as potential decisions regarding the implementation of any novel diagnostic, therapeutic, or preventive measure are based upon a thorough cost–utility assessment. Currently, a number of studies are being conducted in order to improve anti-RSV prophylaxis methods (focusing on both monoclonal antibodies and vaccines) as well as antiviral treatment [ 6 , 7 , 8 , 9 , 10 , 11 ]. The cost-effectiveness analyses initially focused on the costs from a payer’s perspective; however, except for the clinical outcome measures, which include mainly mortality and the frequency of complications, which are major cost-drivers, the awareness of the significance of patient-reported outcome measures (PROMs) and patient-reported experience measures (PREMs) is growing [ 12 ].…”

Section: Introductionmentioning

confidence: 99%

The Impact of RSV Hospitalization on Children’s Quality of Life

Wrotek,

Jackowska

2023

Diseases

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Background: Respiratory syncytial virus (RSV) is one of the most frequent etiological factors of lower respiratory tract infections in children, potentially affecting patients’ quality of life (QoL). We aimed to asses QoL in children under 2 years of age hospitalized due to laboratory-confirmed RSV infection. Methods: A QoL was assessed by parents/tutors with the use of the 100-point visual analog scale and compared against a disease-free period. We evaluated the median utility, QoL loss (reported in days), and quality-adjusted life years (QALY) loss in relation to RSV hospitalization. Results: We included 132 patients aged from 17 days to 24 months (median 3.8 months). The mean utility during the hospitalization varied between 0.418 and 0.952, with a median of 0.679 (95%CI: 0.6–0.757) and median loss of 0.321 [0.243–0.4], which further translated into a loss of 2.2 days (95%CI: 1.6–3.1). The QALY loss varied between 0.526 × 10−3 and 24.658 × 10−3, with a median of 6.03 × 10−3 (95%CI: 4.38–8.48 × 10−3). Based upon the final diagnoses, the highest QALY loss was 6.99 × 10−3 (95%CI: 5.29–13.7 × 10−3) for pneumonia, followed by bronchiolitis—5.96 × 10−3 (4.25–8.41 × 10−3) and bronchitis—4.92 × 10−3 (2.93–6.03 × 10−3); significant differences were observed only between bronchitis and pneumonia (p = 0.0171); the QALY loss was not age-dependent. Although an increasing tendency in the utility score was observed, a strong cumulative effect related to the length of stay was noted until day 13. Conclusions: RSV contributes significantly to the utility deterioration and QALY loss in the case of RSV hospitalization, and the patient-reported data should be used in pharmacoeconomic assessments of the impact of RSV.

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Section: Introductionmentioning

confidence: 99%

The Impact of RSV Hospitalization on Children’s Quality of Life

Wrotek,

Jackowska

2023

Diseases

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“…(1S,2S,4R)-neomenthylamine (7) The material obtained was colorless crystals, with a yield of 78%. The compound was synthesized according to the procedure described earlier in [33].…”

Section: Chemistrymentioning

confidence: 99%

“…Thus, glycyrrhizic acid may exert an antiviral activity against coronaviruses [5,6]. Betulinic acid derivatives exhibit activity against HIV, the coronavirus, and the respiratory syncytial virus [7]. Triterpenoids of the ursane series also exhibit antiviral activity against HIV, the rotavirus, and the influenza virus [8].…”

Section: Introductionmentioning

confidence: 99%

Triterpenic Acid Amides as Potential Inhibitors of the SARS-CoV-2 Main Protease

et al. 2022

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Although the incidence and mortality of SARS-CoV-2 infection has been declining during the pandemic, the problem related to designing novel antiviral drugs that could effectively resist viruses in the future remains relevant. As part of our continued search for chemical compounds that are capable of exerting an antiviral effect against the SARS-CoV-2 virus, we studied the ability of triterpenic acid amides to inhibit the SARS-CoV-2 main protease. Molecular modeling suggested that the compounds are able to bind to the active site of the main protease via non-covalent interactions. The FRET-based enzyme assay was used to reveal that compounds 1e and 1b can inhibit the SARS-CoV-2 main protease at micromolar concentrations.

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“…The F protein is essential for viral entry into the host cell and is considered to be an important target for therapy with low-molecular weight inhibitors, such as JNJ-53718678 [ 6 ] and sisunatovir [ 7 ] ( Figure 1 ), which are under the second phase of clinical trials. Recently, monoterpenoid (–)-borneol and triterpenoid ursolic acid-derived esters 1 [ 8 ] and 2 [ 9 ] have been found to exhibit significant antiviral activity against RSV.…”

Section: Introductionmentioning

confidence: 99%

New Inhibitors of Respiratory Syncytial Virus (RSV) Replication Based on Monoterpene-Substituted Arylcoumarins

et al. 2023

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Respiratory syncytial virus (RSV) causes annual epidemics of respiratory infection. Usually harmless to adults, the RSV infection can be dangerous to children under 3 years of age and elderly people over 65 years of age, often causing serious problems, even death. At present, there are no vaccines and specific chemotherapeutic agents for the treatment of this disease, so the search for low-molecular weight compounds to combat RSV is a challenge. In this work, we have shown, for the first time, that monoterpene-substituted arylcoumarins are efficient RSV replication inhibitors at low micromolar concentrations. The most active compound has a selectivity index of about 200 and acts most effectively at the early stages of infection. The F protein of RSV is a potential target for these compounds, which is also confirmed by molecular docking and molecular dynamics simulation data.

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New triazole-substituted triterpene derivatives exhibiting anti-RSV activity: synthesis, biological evaluation, and molecular modeling

Cited by 5 publications

References 38 publications

The Impact of RSV Hospitalization on Children’s Quality of Life

The Impact of RSV Hospitalization on Children’s Quality of Life

Triterpenic Acid Amides as Potential Inhibitors of the SARS-CoV-2 Main Protease

New Inhibitors of Respiratory Syncytial Virus (RSV) Replication Based on Monoterpene-Substituted Arylcoumarins

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