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antimalarial

NOT Open Access | Synthesis, structure-activity relationship and antimalarial efficacy of 6-chloro-2-arylvinylquinolines

September 23, 2020 - 09:30 -- NOT Open Access
Author(s): 
Huang G, Murillo Solano C, Yuan Y, et al.
Reference: 
J Med Chem. 2020 Sep 22

There is an urgent need to develop new efficacious antimalarials to address the emerging drug-resistant clinical cases. Our previous phenotypic screening identified styrylquinoline UCF501 as a promising antimalarial compound.

Not Open Access | Probing the B- & C-rings of the antimalarial tetrahydro-β-carboline MMV008138 for steric and conformational constraints

September 10, 2020 - 08:33 -- NOT Open Access
Author(s): 
Ding S, Ghavami M, Butler JH, Merino EF, Slebodnick C, Cassera MB, Carlier PR
Reference: 
Bioorg Med Chem Lett. 2020 Sep 5:127520

The antimalarial candidate MMV008138 (1a) is of particular interest because its target enzyme (IspD) is absent in human. To achieve higher potency, and to probe for steric demand, a series of analogs of 1a were prepared that featured methyl-substitution of the B- and C-rings, as well as ring-chain transformations.

Antimalarial artemisinin-based combination therapies (ACT) and COVID-19 in Africa: In vitro inhibition of SARS-CoV-2 replication by mefloquine-artesunate

August 19, 2020 - 09:15 -- Open Access
Author(s): 
Gendrot M, Duflot I, Boxberger M, Delandre O, Jardot P, Le Bideau M, Andreani J, Fonta I, Mosnier J, Rolland C, Hutter S, La Scola B, Pradines B
Reference: 
Int J Infect Dis. 2020 Aug 14:S1201-9712(20)30661-5

At the end of November 2019, a novel coronavirus responsible for respiratory tract infections (COVID-19) emerged in China. Despite drastic containment measures, this virus, known as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), spread in Asia and Europe. The pandemic is ongoing with particular hotspot in Southern Europe and America. Many studies predicted a similar epidemic in Africa as that currently seen in Europe and the United States of America. However, reported data do not confirm these predictions. One of the hypotheses that could explain the later emergence and spread of COVID-19 pandemic in African countries is the use of antimalarial drugs to treat malaria, and more particularly artemisinin-based combination therapy (ACT).

NOT Open Access | The antimalarial activity of indole alkaloids and hybrids

August 17, 2020 - 13:10 -- NOT Open Access
Author(s): 
Li JY, Sun XF, Li JJ, Yu F, Zhang Y, Huang XJ, Jiang FX
Reference: 
Arch Pharm (Weinheim). 2020 Aug 12:e2000131

Malaria, caused by the genus Plasmodium, remains a global public health concern. It is estimated by the World Health Organization that over 40% of the world's population lives in areas at risk for malarial transmission, and around half a million people succumb to this infectious disease annually, which is related to the rapid spread of drug-resistant parasite strains.

Analysis of erythrocyte signalling pathways during Plasmodium falciparum infection identifies targets for host-directed antimalarial intervention

August 13, 2020 - 11:40 -- Open Access
Author(s): 
Adderley JD, John von Freyend S, Jackson SA, Bird MJ, Burns AL, Anar B, Metcalf T, Semblat JP, Billker O, Wilson DW, Doerig C
Reference: 
Nat Commun. 2020 Aug 11;11(1):4015

Intracellular pathogens mobilize host signaling pathways of their host cell to promote their own survival. Evidence is emerging that signal transduction elements are activated in a-nucleated erythrocytes in response to infection with malaria parasites, but the extent of this phenomenon remains unknown. Here, we fill this knowledge gap through a comprehensive and dynamic assessment of host erythrocyte signaling during infection with Plasmodium falciparum.

NOT Open Access | 4-Aminoquinoline-ferrocene Hybrids as Potential Antimalarials

August 5, 2020 - 16:27 -- NOT Open Access
Author(s): 
Nqoro X, Aderibigbe BA
Reference: 
Recent Pat Antiinfect Drug Discov. 2020 Aug 4

Malaria is a deadly disease. It is mostly treated using 4-aminoquinoline derivatives such as chloroquine etc. because it is well tolerated, display low toxicity and after administration, it is rapidly absorbed. The combination of 4-aminoquinoline with other classes of antimalarial drugs has been reported to be an effective approach for the treatment of malaria. Furthermore, some patents reported hybrids 4-aminoquinolines containing ferrocene moiety with potent antimalarial activity.

Heparin Administered to Anopheles in Membrane Feeding Assays Blocks Plasmodium Development in the Mosquito

August 5, 2020 - 16:24 -- Open Access
Author(s): 
Lantero E, Fernandes J, Aláez-Versón CR, Gomes J, Silveira H, Nogueira F, Fernàndez-Busquets X
Reference: 
Biomolecules. 2020 Aug 1;10(8):E1136

Innovative antimalarial strategies are urgently needed given the alarming evolution of resistance to every single drug developed against Plasmodium parasites. The sulfated glycosaminoglycan heparin has been delivered in membrane feeding assays together with Plasmodium berghei-infected blood to Anopheles stephensi mosquitoes.

NOT Open Access | Plasmodium chabaudi-infected mice spleen response to synthesized silver nanoparticles from Indigofera oblongifolia extract

August 5, 2020 - 16:13 -- NOT Open Access
Author(s): 
Al-Quraishy S, Murshed M, Delic D, Al-Shaebi EM, Qasem MAA, Mares MM, Dkhil MA
Reference: 
Lett Appl Microbiol. 2020 Aug 4

Malaria is a worldwide serious-threatening infectious disease caused by Plasmodium and the parasite resistance to antimalarial drugs has confirmed a significant obstacle to novel therapeutic antimalarial drugs. In this article, we assessed the antioxidant and anti-inflammatory activity of nanoparticles prepared from Indigofera oblongifolia extract (AgNPs) against the infection with Plasmodium chabaudi caused in mice spleen.

Organoarsenic Compounds with In Vitro Activity against the Malaria Parasite Plasmodium falciparum

August 5, 2020 - 16:11 -- Open Access
Author(s): 
Basova S, Wilke N, Koch JC, Prokop A, Berkessel A, Pradel G, Ngwa CJ
Reference: 
Biomedicines. 2020 Aug 2;8(8):E260

The rapid development of parasite drug resistance as well as the lack of medications targeting both the asexual and the sexual blood stages of the malaria parasite necessitate the search for novel antimalarial compounds. Eleven organoarsenic compounds were synthesized and tested for their effect on the asexual blood stages and sexual transmission stages of the malaria parasite Plasmodium falciparum using in vitro assays.

Bacillus Calmette-Guérin vaccine, antimalarial, age and gender relation to COVID-19 spread and mortality

August 4, 2020 - 15:06 -- Open Access
Author(s): 
Osama El-Gendy A, Saeed H, Ali AMA, Zawbaa HM, Gomaa D, Harb HS, Madney YM, Osama H, Abdelrahman MA, Abdelrahim MEA
Reference: 
Vaccine. 2020 Jul 31;38(35):5564-5568

COVID-19 is affecting different countries all over the world with great variation in infection rate and death ratio. Some reports suggested a relation between the Bacillus Calmette-Guérin (BCG) vaccine and the malaria treatment to the prevention of SARS-CoV-2 infection. Some reports related infant's lower susceptibility to the COVID-19.

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