Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity

Aguiar, Anna Caroline Campos; Murce, Erika; Cortopassi, Wilian A.; Pimentel, André Silva; Almeida, Margarida; Barros, Daniele C.S.; Guedes, Jéssica S.; Meneghetti, Mário R.; Krettli, Antoniana U.

doi:10.1016/j.ijpddr.2018.10.002

Cited by 75 publications

(58 citation statements)

References 47 publications

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“…Chloroquine is a repurposed drug with great potential to treat COVID-19. Chloroquine has been used to treat malaria for many years [78], with a mechanism that is not well understood against some viral infections. Several possible mechanisms are investigated: Chloroquine can inhibit pH-dependent steps of the replication of several viruses [79], with a potent effect on SARS-CoV infection and spread [80].…”

Section: Antiviral Treatmentsmentioning

confidence: 99%

The origin, transmission and clinical therapies on coronavirus disease 2019 (COVID-19) outbreak – an update on the status

et al. 2020

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An acute respiratory disease, caused by a novel coronavirus (SARS-CoV-2, previously known as 2019-nCoV), the coronavirus disease 2019 (COVID-19) has spread throughout China and received worldwide attention. On 30 January 2020, World Health Organization (WHO) officially declared the COVID-19 epidemic as a public health emergency of international concern. The emergence of SARS-CoV-2, since the severe acute respiratory syndrome coronavirus (SARS-CoV) in 2002 and Middle East respiratory syndrome coronavirus (MERS-CoV) in 2012, marked the third introduction of a highly pathogenic and large-scale epidemic coronavirus into the human population in the twenty-first century. As of 1 March 2020, a total of 87,137 confirmed cases globally, 79,968 confirmed in China and 7169 outside of China, with 2977 deaths (3.4%) had been reported by WHO. Meanwhile, several independent research groups have identified that SARS-CoV-2 belongs to β-coronavirus, with highly identical genome to bat coronavirus, pointing to bat as the natural host. The novel coronavirus uses the same receptor, angiotensin-converting enzyme 2 (ACE2) as that for SARS-CoV, and mainly spreads through the respiratory tract. Importantly, increasingly evidence showed sustained human-to-human transmission, along with many exported cases across the globe. The clinical symptoms of COVID-19 patients include fever, cough, fatigue and a small population of patients appeared gastrointestinal infection symptoms. The elderly and people with underlying diseases are susceptible to infection and prone to serious outcomes, which may be associated with acute respiratory distress syndrome (ARDS) and cytokine storm. Currently, there are few specific antiviral strategies, but several potent candidates of antivirals and repurposed drugs are under urgent investigation. In this review, we summarized the latest research progress of the epidemiology, pathogenesis, and clinical characteristics of COVID-19, and discussed the current treatment and scientific advancements to combat the epidemic novel coronavirus.

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Section: Antiviral Treatmentsmentioning

confidence: 99%

The origin, transmission and clinical therapies on coronavirus disease 2019 (COVID-19) outbreak – an update on the status

et al. 2020

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“…81 Currently, the disease is managed by symptomatic therapy and the Intensive Care Unit is used for the management of patients with severe disease and those that have organ involvement or require intubation. 82 Currently there are more than 80 clinical trials in an effort to find the most appropriate coronavirus treatment. 83 Some of the drugs currently used for the management of COVID-19 include Chloroquine, 83 Remdesivir (GS-5734), 84,85 Lopinavir/ Ritonavir, 86,87,88 and Favipiravir.…”

Section: Therapies Used For the Management Of Covid-19 In Cancer Patimentioning

confidence: 99%

Developing a holistic contingency plan: Challenges and dilemmas for cancer patients during the COVID‐19

et al. 2020

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During the first quarter of 2020 the world is experiencing a pandemic of Severe Acute Respiratory Syndrome‑Coronavirus‑2 (SARS‑CoV‑2), a novel beta coronavirus that is responsible for the 2019 novel coronavirus disease (COVID‐19). The COVID‐19 pandemic revealed that healthcare systems around the world were not prepared to deal with either the direct effects of the pandemic or with the indirect effects that are imposed on the health of patients with chronic disorders such as cancer patients. Some challenges and dilemmas currently faced during the pandemic include the management of cancer patients during the treatment and follow‐up phases, the assessment of the safety of treatments currently used for the management of SARS‑CoV‑2 for use in cancer patients, the development of psychoeducation and emotional support for cancer patients and the safe conduct of clinical trials involving participation of cancer patients. Evidence from the literature supports the need for the urgent development of a holistic contingency plan which will include clear guidelines for the protection and comprehensive care of cancer patients. The implementation of such a plan is expected to have many beneficial effects by mainly minimizing the increased morbidity and mortality of cancer patients that could result as an adverse consequence of the COVID‐19 or future pandemics.

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“…However, all of the tests using these molecules were invalid for COVID-19. By contrast, the best results were obtained with the non-antiviral drug chloroquine, which has been used since the 1950s to treat malaria 22 . Nevertheless, its antiviral mechanism is not well understood; however, we suppose that this compound inhibits pH-dependent steps of the virus replication 23 or interferes with the glycosylation of cellular receptors 24 .…”

Section: Introductionmentioning

confidence: 99%

Potential activity of a selected natural compounds on SARS-CoV-2 RNA-dependent-RNA polymerase, and binding affinity of the receptor-binding domain (RBD)

Altayeb

Bouslama

Abdulhakimc

et al. 2020

Preprint

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Coronavirus disease (COVID-19) is caused by SARS-CoV-2 and represents the causative agent of a potentially lethal disease. COVID-19 has been described as a significant global public health pandemic by the World Health Organization due to its high mortality rate, rapid spread, and the lack of drugs and vaccines for it. Active antiviral drugs are desperately needed to combat the potential return of severe acute respiratory syndrome (SARS).In this study, we selected 39 natural compounds present in plants, algae, and sponges with antiviral activity. Molecular docking was used to screen the compounds’ activity on SARS- CoV-2 RNA-dependent-RNA polymerase, receptor-binding domain (RBD), and the human ACE2 receptor. Compounds with binding energy ≤ -6.5 kcal/mol enter pre-clinical testing using in silco ADME/Tox (absorption, distribution, metabolism, excretion, and toxicity).We found eight potential SARS-CoV-2 inhibitors: (glycyrrhizin, rutin, baicalin, 1, 6-di-O- galloyl-beta-D-glucose, pyropheophorbide A, pheophorbide A, beta-Sitosterol, and vitexin). These outcomes indicate that these compounds could be potential candidates to be utilized in lead optimization for the design and production of the anti-SARS-CoV-2 drug.

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Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity

Cited by 75 publications

References 47 publications

The origin, transmission and clinical therapies on coronavirus disease 2019 (COVID-19) outbreak – an update on the status

The origin, transmission and clinical therapies on coronavirus disease 2019 (COVID-19) outbreak – an update on the status

Developing a holistic contingency plan: Challenges and dilemmas for cancer patients during the COVID‐19

Potential activity of a selected natural compounds on SARS-CoV-2 RNA-dependent-RNA polymerase, and binding affinity of the receptor-binding domain (RBD)

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