4-Aminoquinoline compounds from the Spanish flu to COVID-19

Bazotte, Roberto Barbosa; Hirabara, Sandro Massao; Serdan, Tamires Afonso Duarte; Gritte, Raquel Bragante; Souza‐Siqueira, Talita; Gorjão, Renata; Masi, Laureane Nunes; Antunes, Marina Masetto; Cruzat, Vinícius Fernandes; Pithon-Curi, Tânia Cristina; Curi, Rui

doi:10.1016/j.biopha.2020.111138

Cited by 10 publications

(5 citation statements)

References 78 publications

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“…HCQ generated sense of belief for the treatment and prevention of COVID-19 due to its in vitro virucidal action against SARS-CoV-2 28 . Hydroxychloroquine (HCQ), a less toxic derivative of chloroquine (CQ) is part of the 4-aminoquinoline family compounds 29 . HCQ was initially used as an anti-malarial agent and presently is best recognized as an immunomodulatory and anti-inflammatory agent for the treatment of autoimmune diseases likes rheumatoid arthritis and systemic lupus erythematosus.…”

Section: Discussionmentioning

confidence: 99%

“…HCQ was initially used as an anti-malarial agent and presently is best recognized as an immunomodulatory and anti-inflammatory agent for the treatment of autoimmune diseases likes rheumatoid arthritis and systemic lupus erythematosus. The proposed primary mechanism for anti-viral action of HCQ is alkalinization of endosomes and lysosomes and subsequent rise in pH leading to inhibition of viral nucleic acid replication, protein glycosylation, viral assembly and transportation, and release of new viral particles 28 , 29 . Additionally, HCQ can also block viral uptake by inhibiting the glycosylation of the ACE-2 receptor at the plasma membrane to which viral spike protein binds for cellular entry 29 .…”

Section: Discussionmentioning

confidence: 99%

“…The proposed primary mechanism for anti-viral action of HCQ is alkalinization of endosomes and lysosomes and subsequent rise in pH leading to inhibition of viral nucleic acid replication, protein glycosylation, viral assembly and transportation, and release of new viral particles 28 , 29 . Additionally, HCQ can also block viral uptake by inhibiting the glycosylation of the ACE-2 receptor at the plasma membrane to which viral spike protein binds for cellular entry 29 . Further, the immunomodulatory action can also limit the hyperimmune and inflammatory response of COVID-19 30 , 31 .…”

Section: Discussionmentioning

confidence: 99%

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The ‘myth of Hydroxychloroquine (HCQ) as post-exposure prophylaxis (PEP) for the prevention of COVID-19’ is far from reality

Dhibar

Arora

Chaudhary

et al. 2023

Sci Rep

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The efficacy of Hydroxychloroquine (HCQ) as post-exposure prophylaxis (PEP) for the prevention of COVID-19 was contentious. In this randomized control double-blind clinical trial, asymptomatic individuals with direct contact with laboratory-confirmed COVID-19 cases were randomized into PEP/HCQ (N = 574) and control/placebo (N = 594) group. The PEP/HCQ group received tablet HCQ 400 mg q 12 hourly on day one followed by 400 mg once weekly for 3 weeks, and the control/Placebo group received matching Placebo. The incidence of COVID-19 was similar (p = 0.761) in PEP [N = 24 out of 574, (4.2%)] and control [N = 27 out of 594, (4.5%)] groups. Total absolute risk reduction for the incidence of new-onset COVID-19 was -0.3% points with an overall relative risk of 0.91 (95% confidence interval, 0.52 to 1.60) and the number needed to treat (NNT) was 333 to prevent the incident of one case of COVID-19. The study found that, PEP with HCQ was not advantageous for the prevention of COVID-19 in asymptomatic individuals with high risk for SARS-CoV-2 infection. Though HCQ is a safer drug, the practice of irrational and indiscriminate use of HCQ for COVID-19 should be restrained with better pharmacovigilance.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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The ‘myth of Hydroxychloroquine (HCQ) as post-exposure prophylaxis (PEP) for the prevention of COVID-19’ is far from reality

Dhibar

Arora

Chaudhary

et al. 2023

Sci Rep

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“…This study concluded that quinine has an antiviral effect against influenza viruses by consistently slowing the course of infection with the influenza virus. 38 Quinine’s antiviral activity has also been demonstrated in several other viruses, such as H1N1 39 , Influenza A virus (IAV), Human Immunodeficiency Virus (HIV), Zika virus, Ebola and dengue. 40 , 41 In addition, the antiviral effect of quinine was described by Baroni at al, who evaluated QS in HaCat HSV-1 infected cells.…”

Section: Methodsmentioning

confidence: 99%

Potential of Quinine Sulfate for COVID-19 Treatment and Its Safety Profile: Review

Latarissa¹,

Barliana²,

Meiliana³

et al. 2021

CPAA

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The coronavirus disease 2019 (COVID-19) pandemic is currently the largest and most serious health crisis in the world. There is no definitive treatment for COVID-19. Vaccine administration has begun in various countries, but no vaccine is 100% effective. Some people are not protected after vaccination, and there are some groups of people who cannot be vaccinated therefore, research on COVID-19 treatment still needs to be done. Of the several drugs under study, chloroquine (CQ) and hydroxychloroquine (HCQ) are quite controversial, although they have good activity against SARS-CoV-2, both drugs have serious side effects. Indonesia with its wealth of natural ingredients has one potential compound, quinine sulfate (QS), which has the same structure and activity as CQ and HCQ and a better safety profile. The aim of this article was to review the potential of QS against the SARS-Cov-2 virus and outline its safety profile. We conclude that QS has the potential to be developed as a COVID-19 treatment with a better safety profile than that of CQ and HCQ.

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“…Therefore, continuous clinical investigations were carried out using two approved drugs of 4‐aminoquinoline scaffold for example, chloroquine (CQ) and hydroxychloroquine (HCQ). [ 33 ] Due to less toxicity and high solubility of hydroxychloroquine as compared to chloroquine, it was widely used during the COVID‐19 pandemic as an antiviral agent for the treatment and further investigations. Reported studies showed in vitro activity of HCQ against SARS‐CoV‐2.…”

Section: Anti‐infective Potential Of 4‐substituted Quinolinesmentioning

confidence: 99%

Spotlight on 4‐substituted quinolines as potential anti‐infective agents: Journey beyond chloroquine

Goyal

Kharkwal

Piplani

et al. 2022

Archiv der Pharmazie

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Continued emerging resistance of pathogens against the clinically approved candidates and their associated limitations continuously demand newer agents having better potency with a more suited safety profile. Quinoline nuclei containing scaffolds of natural and synthetic origin have been documented for diverse types of pharmacological activities, and a number of drugs are clinically approved. In the present review, we unprecedentedly covered the biological potential of 4-substituted quinoline and elaborated a rationale for its special privilege to afford the significant number of approved clinical drugs, particularly against infectious pathogens. Compounds with 4-substituted quinoline are well documented for antimalarial activity, but in the last two decades, they have been extensively explored for activity against cancer, tuberculosis, and several other pathogens including viruses, bacteria, fungi, and other infectious pathogens. In the present study, the anti-infective spectrum of this scaffold is discussed against viruses, mycobacteria, malarial parasites, and fungal and bacterial strains, along with recent updates in this area, with special emphasis on the structure-activity relationship.

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4-Aminoquinoline compounds from the Spanish flu to COVID-19

Abstract: Graphical abstract Mechanisms of action of 4-aminoquinoline compounds on viral infection.

Cited by 10 publications

References 78 publications

The ‘myth of Hydroxychloroquine (HCQ) as post-exposure prophylaxis (PEP) for the prevention of COVID-19’ is far from reality

The ‘myth of Hydroxychloroquine (HCQ) as post-exposure prophylaxis (PEP) for the prevention of COVID-19’ is far from reality

Potential of Quinine Sulfate for COVID-19 Treatment and Its Safety Profile: Review

Spotlight on 4‐substituted quinolines as potential anti‐infective agents: Journey beyond chloroquine

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