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antimalarial

Modular synthesis of antimalarial quinoline-based PGM metallarectangles

October 16, 2021 - 12:18 -- Open Access
Author(s): 
Golding TM, Mbaba M, Smith GS
Reference: 
Dalton Trans. 2021 Oct 11

A new ditopic, quinoline-based ligand L (7-chloro-4-(pyridin-4-yl)quinoline) was synthesized via a Suzuki cross-coupling reaction. The ligand was utilized to synthesize the corresponding half-sandwich iridium(III) and ruthenium(II) binuclear complexes (1c and 1d) and the subsequent metallarectangles (2c, 2d, 3c, and 3d), via [2 + 2] coordination-driven self-assembly. Single-crystal X-ray diffraction confirmed the proposed molecular structure of the binuclear complex [{IrCl2(Cp*)}2(μ-L)] (1c) and DFT calculations were used to predict the optimized geometry of the rectangular nature of [{Ir(μ-Cl)(Cp*)}4(μ-L)2](CF3SO3)4 (2c).

NOT Open Access | Suppressive, curative, and prophylactic potentials of an antimalarial polyherbal mixture and its individual components in Plasmodium berghei-Infected mice

September 23, 2021 - 11:33 -- NOT Open Access
Author(s): 
Alaribe SC, Oladipupo AR, Uche GC, Onumba MU, Ota D, Awodele O, Oyibo WA
Reference: 
J Ethnopharmacol. 2021 Sep 15;277:114105

Malaria remains one of the most prevalent infectious diseases in tropical regions of the world, particularly in sub-Saharan Africa, where it remains epidemiologically holoendemic. The absence of effective vaccines and Plasmodium resistance to antimalarial drugs have been the major challenges to malaria control measures. An alternative strategy could be the application of validated and standardized herbal formulations.

Prioritization of Molecular Targets for Antimalarial Drug Discovery

September 18, 2021 - 04:12 -- Open Access
Author(s): 
Forte B, Ottilie S, Gilbert IH, et al.
Reference: 
ACS Infect Dis. 2021 Sep 15

There is a shift in antimalarial drug discovery from phenotypic screening toward target-based approaches, as more potential drug targets are being validated in Plasmodium species. Given the high attrition rate and high cost of drug discovery, it is important to select the targets most likely to deliver progressible drug candidates. In this paper, we describe the criteria that we consider important for selecting targets for antimalarial drug discovery.

Structural characterization of the Plasmodium falciparum lactate transporter PfFNT alone and in complex with antimalarial compound MMV007839 reveals its inhibition mechanism

September 14, 2021 - 09:25 -- Open Access
Author(s): 
Peng X, Wang N, Deng D, et al.
Reference: 
PLoS Biol. 2021 Sep 9;19(9):e3001386

Plasmodium falciparum, the deadliest causal agent of malaria, caused more than half of the 229 million malaria cases worldwide in 2019. The emergence and spreading of frontline drug-resistant Plasmodium strains are challenging to overcome in the battle against malaria and raise urgent demands for novel antimalarial agents. The P. falciparum formate–nitrite transporter (PfFNT) is a potential drug target due to its housekeeping role in lactate efflux during the intraerythrocytic stage.

To what extent are the antimalarial markets in African countries ready for a transition to triple artemisinin-based combination therapies

September 1, 2021 - 17:12 -- Open Access
Author(s): 
de Haan F, Bolarinwa OA, Amaratunga C, et al.
Reference: 
PLoS One. 2021 Aug 31;16(8):e0256567

Triple artemisinin-based combination therapies (TACTs) are being developed as a response to artemisinin and partner drug resistance in the treatment of falciparum malaria in Southeast Asia. In African countries, where current artemisinin-based combination therapies (ACTs) are still effective, TACTs have the potential to benefit the larger community and future patients by mitigating the risk of drug resistance. This study explores the extent to which the antimalarial drug markets in African countries are ready for a transition to TACTs.

NOT Open Access | Antimalarial Activities of (Z)-2-(Nitroheteroarylmethylene)-3(2H)-Benzofuranone Derivatives: In Vitro and In Vivo Assessment and β-Hematin Formation Inhibition Activity

August 18, 2021 - 17:05 -- NOT Open Access
Author(s): 
Navidpour L, Chibale K, Esmaeili S, Ghiaee A, Hadj-Esfandiari N, Irani M, Ahmadi Koulaei S, Yassa N
Reference: 
Antimicrob Agents Chemother. 2021 Aug 17;65(9):e0268320

A series of (Z)-2-(nitroheteroarylmethylene)-3(2H)-benzofuranones possessing nitroheteroaryl groups of nitroimidazole, nitrofuran, and nitrothiophene moieties was screened for antiplasmodium activity against a drug-sensitive strain (3D7 strain) and a multidrug-resistant (chloroquine [CQ] and pyrimethamine) strain (K1 strain) of Plasmodium falciparum. 5-Nitroimidazole and 4-nitroimidazole analogs were highly selective and active against resistant parasites, while 5-nitrofuran and 5-nitrothiophene derivatives were more potent against the 3D7 strain than against the K1 strain.

NOT Open Access | Linking microbiota composition with antimalarial antibody response

August 17, 2021 - 14:34 -- NOT Open Access
Author(s): 
Romoli O, Mancio-Silva L, Gendrin M
Reference: 
Trends Parasitol. 2021 Aug 11:S1471-4922(21)00172-0

Microbiota composition recently arose as a factor correlating with malaria infection. Mandal et al. showed, via cecal transplant and antibacterial treatment, that the mouse microbiota modulates parasitemia by affecting spleen germinal centers where B cells are matured. They further identified correlations between microbiota composition and malaria severity in Ugandan children.

NOT Open Access | Antimalarial chemoprophylaxis and treatment in the United States: Limited access and extreme price variability

August 11, 2021 - 15:00 -- NOT Open Access
Author(s): 
Frosch AE, Thielen BK, Alpern JD, Walz EJ, Volkman HR, Smith M, Wanduragala D, Holder W, Boumi AE, Stauffer WM
Reference: 
J Travel Med. 2021 Aug 3:taab117

To evaluate if cost and availability of antimalarials are barriers to malaria chemoprophylaxis and treatment, we surveyed retail pharmacies in Minneapolis/Saint Paul and New York City on the price and stocking of antimalarials.

NOT Open Access | Antimalarial drug discovery: from quinine to the most recent promising clinical drug candidates

August 11, 2021 - 14:55 -- NOT Open Access
Author(s): 
Tisnerat C, Dassonville-Klimpt A, Gosselet F, Sonnet P
Reference: 
Curr Med Chem. 2021 Aug 3

Malaria is a tropical threatening disease caused by Plasmodium parasites, resulting in 409,000 deaths in 2019. The delay of mortality and morbidity has been compounded by the widespread of drug resistant parasites from Southeast Asia since two decades. The emergence of artemisinin-resistant Plasmodium in Africa, where most cases are accounted, highlights the urgent need for new medicines.

Not Open Access | Artemisinin inspired synthetic endoperoxide drug candidates: Design, synthesis, and mechanism of action studies

August 10, 2021 - 17:46 -- NOT Open Access
Author(s): 
Woodley CM, Amado PSM, Cristiano MLS, O'Neill PM
Reference: 
Med Res Rev. 2021 Aug 6

Artemisinin combination therapies (ACTs) have been used as the first-line treatments against Plasmodium falciparum malaria for decades. Recent advances in chemical proteomics have shed light on the complex mechanism of action of semi-synthetic artemisinin (ARTs), particularly their promiscuous alkylation of parasite proteins via previous heme-mediated bioactivation of the endoperoxide bond. Alarmingly, the rise of resistance to ART in South East Asia and the synthetic limitations of the ART scaffold have pushed the course for the necessity of fully synthetic endoperoxide-based antimalarials.

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