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Not Open Access | 2-Methylthio-N7-methyl-cis-zeatin, a new antimalarial natural product isolated from a Streptomyces culture

December 28, 2021 - 20:46 -- NOT Open Access
Lopez JAV, Nogawa T, Yoshida K, Futamura Y, Osada H
Biosci Biotechnol Biochem. 2021 Dec 22;86(1):31-36

2-Methylthio-N7-methyl-cis-zeatin (1) was isolated from the culture broth of Streptomyces sp. 80H647 along with 2 known purine derivatives, 5'-methylthioinosine (2) and AT-265 (dealanylascamycin, 3).

NOT Open Access | Recent contributions of quinolines to antimalarial and anticancer drug discovery research

December 27, 2021 - 10:38 -- NOT Open Access
Van de Walle T, Cools L, Mangelinckx S, D'hooghe M
Eur J Med Chem. 2021 Dec 15;226:113865

Quinoline, a privileged scaffold in medicinal chemistry, has always been associated with a multitude of biological activities. Especially in antimalarial and anticancer research, quinoline played (and still plays) a central role, giving rise to the development of an array of quinoline-containing pharmaceuticals in these therapeutic areas. However, both diseases still affect millions of people every year, pointing to the necessity of new therapies.

Not Open Access | New insights into antimalarial chemopreventive activity of antifolates

December 27, 2021 - 10:36 -- NOT Open Access
Pethrak C, Posayapisit N, Jupatanakul N, et al.
Antimicrob Agents Chemother. 2021 Dec 20:AAC0153821

Antifolates targeting dihydrofolate reductase (DHFR) are antimalarial compounds that have long been used for malaria treatment and chemoprevention (inhibition of infection from mosquitoes to humans). Despite their extensive applications, the thorough understanding of antifolate activity against hepatic malaria parasites, especially resistant parasites, have yet to be achieved.

Modular synthesis of antimalarial quinoline-based PGM metallarectangles

October 16, 2021 - 12:18 -- Open Access
Golding TM, Mbaba M, Smith GS
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
Alaribe SC, Oladipupo AR, Uche GC, Onumba MU, Ota D, Awodele O, Oyibo WA
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
Forte B, Ottilie S, Gilbert IH, et al.
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
Peng X, Wang N, Deng D, et al.
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
de Haan F, Bolarinwa OA, Amaratunga C, et al.
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
Navidpour L, Chibale K, Esmaeili S, Ghiaee A, Hadj-Esfandiari N, Irani M, Ahmadi Koulaei S, Yassa N
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
Romoli O, Mancio-Silva L, Gendrin M
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.


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