One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activity

Botta, Lorenzo; Maccari, Giorgio; Calandro, Pierpaolo; Tiberi, Marika; Brai, Annalaura; Zamperini, Claudio; Canducci, Filippo; Chiariello, Mario; Martí‐Centelles, Rosa; Falomir, Eva; Cardá, Miguel

doi:10.1016/j.bmcl.2017.03.097

Cited by 9 publications

(6 citation statements)

References 15 publications

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“…In our previous papers we reported some rhodanine and aminothiazolone derivatives endowed with nanomolar activities against HIV-1 infected cells [8–10]. In a recent work, we showed that our compounds were also active against HSV-1/2, while they were completely ineffective against HPV, a nonenveloped virus [11].…”

Section: Introductionmentioning

confidence: 83%

Novel broad spectrum virucidal molecules against enveloped viruses

et al. 2018

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Viral infections are an important cause of death worldwide. Unfortunately, there is still a lack of antiviral drugs or vaccines for a large number of viruses, and this represents a remarkable challenge particularly for emerging and re-emerging viruses. For this reason, the identification of broad spectrum antiviral compounds provides a valuable opportunity for developing efficient antiviral therapies. Here we report on a class of rhodanine and thiobarbituric derivatives displaying a broad spectrum antiviral activity against seven different enveloped viruses including an HSV-2 acyclovir resistant strain with favorable selectivity indexes. Due to their selective action on enveloped viruses and to their lipid oxidation ability, we hypothesize a mechanism on the viral envelope that affects the fluidity of the lipid bilayer, thus compromising the efficiency of virus-cell fusion and preventing viral entry.

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Section: Introductionmentioning

confidence: 83%

Novel broad spectrum virucidal molecules against enveloped viruses

et al. 2018

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“…Scientists in previous studies presented several methods for the treatment of HIV in the early stages to prevent entry into the cell [81][82][83]. In fact, this can be attributed to increasing the availability of antiviral agents in effective and important preparations.…”

Section: Antiviral Activitymentioning

confidence: 99%

A conceptual review of rhodanine: current applications of antiviral drugs, anticancer and antimicrobial activities

Mousavi

Zarei

Hashemi

et al. 2019

Artificial Cells, Nanomedicine, and Biotechnology

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Rhodanines are accepted as advantaged heterocycles in medicinal chemistry as one of the 4-thiazolidinones subtypes. The aim of this paper is to analyze the features of rhodanine and its application in pharmacy and medicine. Some of the properties of rhodanine such as antiviral, anticancer, antimicrobial, and drug discovery have recently been reported. Although there are still vague points in the structure and mechanism of polymerization of this substance, there is a significant increase in the use of rhodanine in medicine. In this review paper, it can be said that we have provided a general overview of the recent advances in the rhodanine-based material which its application is more in the field of drug discovery and anticancer activity. The review starts with a summary of the antiviral activity of rhodanine-based materials and nanocomposites in general. Then in the next step, the detailed description is followed on their applications in the fields of anticancer activity, drug discovery, and an innovative type of rhodanine (RH) and thiohydantoin (TH) derivatives were created and combined in order to recognize tau pathology in the brains of patients with Alzheimer's disease (AD). Through this review, we hope to promote rhodanine and its role in medicine and pharmacy becomes more prominent.

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“…Rhodanines are accepted as advantaged heterocycles in medicinal chemistry as one of the 4-thiazolidinones subtypes [7][8][9][10][11]. Thioxo-thiazolidinone (Rhodanine) and its derivatives [12,13] are reported to have a broad spectrum of biological activities such as antibacterial [14][15][16][17][18][19], antifungal [20][21][22], anti-diabetic [23,24], anti-tubercular [25][26][27] anticancer [28,29] anti-HIV [30][31][32][33][34][35][36][37][38] and antimalarial [39]. Rhodanine derivatives have been investigated for Alzheimer's disease also [40,41].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Antimicrobial Studies of 5-Benzylidene Substituted Rhodanine Containing Heterocycles

Mathew

Saraswati

Lal

et al. 2021

Int J Pharm Pharm Sci

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Objective: The principal objective of the study was to synthesize and evaluate the biological activities of a novel class of 5-benzylidene substituted rhodanine derivatives as antimicrobial agents. Methods: All the synthesized compounds (D1-D10) were screened for their antimicrobial activities using microdilution methods as per the reported procedure. All compounds were evaluated as potential antimicrobial agents against gram-positive bacteria: Bacillus cereus, Staphylococcus aureus, gram negative bacteria: Escherichia coli Pseudomonas aeruginosa and Klebsiella pneumoniae Fungal cultures used in the study were Aspergillus niger, Candida albicans, Candida parapsilosis, Candida tropicalis and Candida glabrata. Results: Compound D6 showed good antifungal activity in the MIC range 16μg/ml against Candida tropicalis and Compound D10 showed good antifungal activity in the MIC range 16μg/ml against Candida glabrata. Compounds D2 and D5 showed good antibacterial activity at 32μg/ml. all the other compounds showed moderate antibacterial activity. Conclusion: Based on the above results, it can be concluded that the compounds may lead to the development of more potent antimicrobial drug candidates in the near future.

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One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activity

Cited by 9 publications

References 15 publications

Novel broad spectrum virucidal molecules against enveloped viruses

Novel broad spectrum virucidal molecules against enveloped viruses

A conceptual review of rhodanine: current applications of antiviral drugs, anticancer and antimicrobial activities

Design, Synthesis and Antimicrobial Studies of 5-Benzylidene Substituted Rhodanine Containing Heterocycles

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