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NOT Open Access | Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials

May 13, 2020 - 14:01 -- NOT Open Access
Kancharla P, Dodean RA, Kelly JX, et al.
J Med Chem. 2020 May 11

The global impact of malaria remains staggering despite extensive efforts to eradicate the disease. With increasing drug resistance and the absence of a clinically available vaccine, there is an urgent need for novel, affordable, and safe drugs for prevention and treatment of malaria.

Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway

April 15, 2020 - 14:19 -- Open Access
LaMonte GM, Rocamora F, Winzeler EA, et al.
Nat Commun. 2020 Apr 14;11(1):1780

A promising new compound class for treating human malaria is the imidazolopiperazines (IZP) class. IZP compounds KAF156 (Ganaplacide) and GNF179 are effective against Plasmodium symptomatic asexual blood-stage infections, and are able to prevent transmission and block infection in animal models.

Genetic ablation of the mitoribosome in the malaria parasite Plasmodium falciparum sensitizes it to antimalarials that target mitochondrial functions

April 13, 2020 - 15:04 -- Open Access
Ling L, Mulaka M, Munro J, Dass S, Mather MW, Riscoe MK, Llinás M, Zhou J, Ke H
J Biol Chem. 2020 Apr 9. pii: jbc.RA120.012646

The mitochondrion of malaria parasites contains several clinically validated drug targets. Within Plasmodium spp., the causative agents of malaria, the mitochondrial DNA (mtDNA) is only 6 kb long, being the smallest mitochondrial genome among all eukaryotes.

NOT Open Access | Plasmodium stage-selective antimalarials from Lophira lanceolata stem bark

March 23, 2020 - 14:53 -- NOT Open Access
Soré H, Lopatriello A, Ebstie YA, Tenoh Guedoung AR, Hilou A, Pereira JA, Kijjoa A, Habluetzel A, Taglialatela-Scafati O
Phytochemistry Volume 174, June 2020, 112336

Targeting the transmissible stages of the Plasmodium parasite that develop in the human and mosquito host is a crucial strategy for malaria control and elimination. Medicinal plants offer a prolific source for the discovery of new antimalarial compounds. The recent identification of the gametocytocidal activity of lophirone E, obtained from the African plant Lophira lanceolata (Ochnaceae), inspired the evaluation of the plant also against early sporogonic stages of the parasite development.

NOT Open Access | Effect of Adding Azithromycin to the Antimalarials used for Seasonal Malaria Chemoprevention on the Nutritional Status of African Children

March 18, 2020 - 14:37 -- NOT Open Access
Gore-Langton GR, Cairns M, Ouedraogo JB, et al.
Trop Med Int Health. 2020 Mar 12

Mass administration of azithromycin has reduced mortality in children in sub‐Saharan Africa but its mode of action is not well characterised. A recent trial found that azithromycin given alongside seasonal malaria chemoprevention was not associated with a reduction in mortality or hospital admissions in young children. We investigated the effect of azithromycin on the nutritional status of children enrolled in this study.

A Single-Dose Combination Study with the Experimental Antimalarials Artefenomel and DSM265 To Determine Safety and Antimalarial Activity against Blood-Stage Plasmodium falciparum in Healthy Volunteers

December 23, 2019 - 16:04 -- Open Access
McCarthy JS, Rückle T, Elliott SL, Ballard E, Collins KA, Marquart L, Griffin P, Chalon S, Möhrle JJ
Antimicrob Agents Chemother. 2019 Dec 20;64(1). pii: e01371-19.

Artefenomel and DSM265 are two new compounds that have been shown to be well tolerated and effective when administered as monotherapy malaria treatment. This study aimed to determine the safety, pharmacokinetics, and pharmacodynamics of artefenomel and DSM265 administered in combination to healthy subjects in a volunteer infection study using the Plasmodium falciparum-induced blood-stage malaria model. Thirteen subjects were inoculated with parasite-infected erythrocytes on day 0 and received a single oral dose of artefenomel and DSM265 on day 7.

NOT Open Access | 6-Hydrophobic aromatic substituent pyrimethamine analogues as potential antimalarials for pyrimethamine-resistant Plasmodium falciparum

December 16, 2019 - 16:55 -- NOT Open Access
Saepua S, Sadorn K, Vanichtanankul J, Anukunwithaya T, Rattanajak R, Vitsupakorn D, Kamchonwongpaisan S, Yuthavong Y, Thongpanchang C
Bioorganic & Medicinal Chemistry Volume 27, Issue 24, 15 December 2019, 115158

The series of des-Cl (unsubstituted) and m-Cl phenyl analogues of PYR with various flexible 6-substituents were synthesized and studied for the binding affinities with highly resistant quadruple mutant (QM) DHFR. The derivatives carrying 4 atoms linker with a terminal carboxyl substituted on the aromatic ring exhibited good inhibition to the QM enzyme and also showed effective antimalarial activities against resistant P. falciparum bearing the mutant enzymes with relatively low cytotoxicity to mammalian cells.

NOT Open Access |Recent advances in transmission-blocking drugs for malaria elimination

December 2, 2019 - 15:10 -- NOT Open Access
Wadi I, Nath M, Anvikar AR, Singh P, Sinha A.
Future Med Chem. 2019 Nov 29.

The scientific community worldwide has realized that malaria elimination will not be possible without development of safe and effective transmission-blocking interventions. Primaquine, the only WHO recommended transmission-blocking drug, is not extensively utilized because of the toxicity issues in G6PD deficient individuals.

Improving Methods for Analyzing Antimalarial Drug Efficacy Trials: Molecular Correction Based on Length-Polymorphic Markers msp-1, msp-2, and glurp

September 9, 2019 - 16:25 -- Open Access
S. Jones, K. Kay, E. M. Hodel, S. Chy, A. Mbituyumuremyi, A. Uwimana, D. Menard, I. Felger and I. Hastings
Antimicrob. Agents Chemother. August 2019 63:e00590-19

Drug efficacy trials monitor the continued efficacy of front-line drugs against falciparum malaria.

NOT Open Access | Dihydroartemisinin, an antimalarial drug, induces absent in melanoma 2 inflammasome activation and autophagy in human hepatocellular carcinoma HepG2215 cells

June 3, 2019 - 15:24 -- NOT Open Access
Xinli Shi, Li Wang, Laifeng Ren, Jianchun Li, Shenghao Li, Qingzhuo Cui, Sheng Li
Phytotherapy Research, Volume33, Issue5 May 2019 Pages 1413-1425

As an effective antimalarial drug, Dihydroartemisinin (DHA) is readily isolated from the traditional Chinese medicine of Artemisia annua.


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