Synthesis and biological evaluation of novel rhodanine-based structures with antiviral activity towards HHV-6 virus

Gentili, Valentina; Turrin, Giulia; Marchetti, Paolo; Rizzo, Sabrina; Schiuma, Giovanna; Beltrami, Silvia; Cristofori, Virginia; Illuminati, Davide; Compagnin, Greta; Trapella, Claudio; Rizzo, Roberta; Bortolotti, Daria; Fantinati, Anna

doi:10.1016/j.bioorg.2021.105518

Cited by 4 publications

(3 citation statements)

References 39 publications

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“…61 No antiviral drug has been approved or systematically investigated for treatment of HHV-6 infection, however HHV-6 fusion inhibitors with a rhodamine structure were tested in human cells. 157 Integrated Rationale for the Spectrum of EBV Infection Sequalae…”

Section: Treatment Of Cns Disorders Associated With Possible Co-infec...mentioning

confidence: 99%

Treatment Options for Epstein-Barr Virus-Related Disorders of the Central Nervous System

Andersen¹,

Ernberg²,

Hedström³

2023

IDR

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Epstein-Barr virus (EBV), a causative agent for several types of lymphomas and mucosal cancers, is a human lymphotropic herpesvirus with the capacity to establish lifelong latent infection. More than 90% of the human population worldwide is infected. The primary infection is usually asymptomatic in childhood, whereas infectious mononucleosis (IM) is common when the infection occurs in adolescence. Primary EBV infection, with or without IM, or reactivation of latent infection in immunocompromised individuals have been associated with a wide range of neurologic conditions, such as encephalitis, meningitis, acute disseminated encephalomyelitis, and cerebellitis. EBV is also involved in malignant lymphomas in the brain. An increasing number of reports on EBV-related disorders of the central nervous system (CNS) including the convincing association with multiple sclerosis (MS) have put in focus EBV-related conditions beyond its established link to malignancies. In this review, we present the clinical manifestations of EBVrelated CNS-disorders, put them in the context of known EBV biology and focus on available treatment options and future therapeutic approaches.

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Section: Treatment Of Cns Disorders Associated With Possible Co-infec...mentioning

confidence: 99%

Treatment Options for Epstein-Barr Virus-Related Disorders of the Central Nervous System

Andersen¹,

Ernberg²,

Hedström³

2023

IDR

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“…Among various compounds, 258a was chosen as lead, and further modification and subsequent evaluation of compounds possessing a peculiar combination of hydrophilic and hydrophobic substituents at the rhodanine core adjudged molecule 258e as the most potent derivative among them. Further, the molecule showed no significant toxicity, and the effects lasted up to 7 days post‐treatment (Gentili et al, 2022).…”

Section: Biological Spectrum Of Rhodanine Derivativesmentioning

confidence: 99%

Rhodanine derivatives: An insight into the synthetic and medicinal perspectives as antimicrobial and antiviral agents

et al. 2022

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Rhodanine or 2-Thioxothiazolidin-4-one is a privileged heterocyclic compound offering a wide opportunity for structural modification, lead development, and modification. It is one of the highly decorated scaffolds in the drug discovery process. Rhodanine derivatives possess a plethora of biological activities due to their ability to interact with a diverse range of protein targets, which provide tremendous opportunities to discover new drugs with different modes of action. The most common strategy for developing novel rhodanine derivatives is the introduction of structurally diverse substituents at the C-5 or N-3, or both positions. Since the inception of Epralestat into the market in 1992, the exploration of rhodanine-3acetic acids has led to the development of novel leads against different biological targets such as MRSA, HHV-6, Mycobacterial tuberculosis, dengue, etc. In the current pandemic era, some rhodanine compounds have been explored against SARS-CoV-2. In recent years, rhodanine and its derivatives have witnessed significant progress in developing new drug leads as potential antimicrobial and antiviral agents. Different synthetic methodologies and recent developments in the medicinal chemistry of rhodanine derivatives, including biological activities, their mechanistic aspects, structure-activity relationships, and in silico findings, have been compiled in the present review. This article will benefit the scientific community and offer perspectives on how these scaffolds as privileged structures might be exploited in the future for rational design and discovery of rhodaninebased bio-active molecules.

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“…49 Compounds that inhibit SrtA may function as potent anti-infective agents, as this enzyme is responsible for cell wall virulence factors. In study 50 potential fusion intermediates inhibitors based on the rhodanine structure were synthetized. The obtained derivatives were tested for cytotoxicity and for antiviral activity in human cells infected with HHV6.…”

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confidence: 99%

Synthesis and biological activity of rhodanine-furan conjugates: A review

Matiichuk,

Drapak,

Darmograi

et al. 2024

10.5267/j.ccl

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Rhodanines are recognized as privileged heterocycles in medicinal chemistry. The main achievements include the development of drug-like molecules with numerous biological activities as well as approved drugs. The Furan nucleus is considered one of the promising heterocyclic cores in medicinal chemistry that showed numerous ranges of activity. The combination of several heterocycles in a one molecule commonly provides much more interest in the enhanced activity profile of its analogs than their parent separate constituents. Such conjugates are promising objects for modern medicinal chemistry. In this review paper recent advances in the synthesis and biological activities rhodanine-furan conjugates which its application in the different field of drug discovery.

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Synthesis and biological evaluation of novel rhodanine-based structures with antiviral activity towards HHV-6 virus

Cited by 4 publications

References 39 publications

Treatment Options for Epstein-Barr Virus-Related Disorders of the Central Nervous System

Treatment Options for Epstein-Barr Virus-Related Disorders of the Central Nervous System

Rhodanine derivatives: An insight into the synthetic and medicinal perspectives as antimicrobial and antiviral agents

Synthesis and biological activity of rhodanine-furan conjugates: A review

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