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antimalarial activity

Chemoprotective Antimalarial Activity of P218 against Plasmodium falciparum: A Randomized, Placebo-Controlled Volunteer Infection Study

February 10, 2021 - 09:44 -- Open Access
Author(s): 
Chughlay MF, El Gaaloul M, Chalon S, et al.
Reference: 
Am J Trop Med Hyg. 2021 Feb 8:tpmd201165

P218 is a highly selective dihydrofolate reductase inhibitor with potent in vitro activity against pyrimethamine-resistant Plasmodium falciparum. This single-center, randomized, double-blind, placebo-controlled phase Ib study evaluated P218 safety and chemoprotective efficacy in a P. falciparum sporozoite (PfSPZ) volunteer infection study (VIS). Consecutive dose safety and tolerability were evaluated (cohort 1), with participants receiving two oral doses of P218 1,000 mg 48 hours apart (n = 6), or placebo (n = 2). P218 chemoprotective efficacy was assessed (cohorts 2 and 3) with direct venous inoculation of 3,200 aseptic, cryopreserved PfSPZ (NF54 strain) followed 2 hours later with two P218 doses of 1,000 mg (cohort 2, n = 9) or 100 mg (cohort 3, n = 9) administered 48 hours apart, or placebo (n = 6).

NOT Open Access | A Concise Total Synthesis of Dehydroantofine and the Antimalarial Activity against Chloroquine-Resistant P. falciparum

January 26, 2021 - 15:09 -- NOT Open Access
Author(s): 
Yamasaki N, Iwasaki I, Sakumi K, Hokari R, Ishiyama A, Iwatsuki M, Nakahara M, Higashibayashi S, Sugai T, Imagawa H, Kubo M, Fukuyama Y, Ōmura S, Yamamoto H
Reference: 
Chemistry. 2021 Jan 2

A total synthesis of dehydroantofine was achieved by employing a novel, regioselective azahetero Diels-Alder reaction of the easily accessible 3,5-dichloro-2 H -1,4-oxazin-2-one with 4-ethynyl-1,2-dimethoxybenzene as a key step.

NOT Open Access | In vitro evaluation and molecular dynamics, DFT guided investigation of antimalarial activity of ethnomedicinally used Coptis teeta Wall

January 20, 2021 - 06:16 -- NOT Open Access
Author(s): 
Goswami AK, Sharma HK, Gogoi N, Kashyap A, Gogoi BJ
Reference: 
Comb Chem High Throughput Screen. 2021 Jan 17

Malaria is caused by different species of Plasmodium; among which P. falciparum is the most severe. Coptis teeta is an ethnomedicinal plant of enormous importance for tribes of north east India.

NOT Open Access | Formulation development and characterization of Lumefantrine nanosuspension for enhanced antimalarial activity

January 6, 2021 - 12:59 -- NOT Open Access
Author(s): 
Shah R, Soni T, Shah U, Suhagia BN, Patel MN, Patel T, Gabr GA, Gorain B, Kesharwani P
Reference: 
J Biomater Sci Polym Ed. 2020 Dec 30:1-18

Variable and low oral bioavailability (4-11%) of lumefantrine (LUF), an anti-malarial agent, is characterized by very low solubility in aqueous vehicle. Thus, the present study was intended to formulate lyophilized nanosuspensions of LUF to resolve its solubility issues for the improvement of oral bioavailability. A three level 32 factorial design was applied to analyze the influence of independent variables, concentration of polysorbate 80 (X1) and sonication time (X2) on the responses for dependent variables, particle size (Y1) and time to 90% release of LUF (t90) (Y2).

NOT Open Access | In silico study, synthesis, and evaluation of the antimalarial activity of hybrid dimethoxy pyrazole 1,3,5-triazine derivatives

December 23, 2020 - 09:35 -- NOT Open Access
Author(s): 
Gogoi P, Shakya A, Ghosh SK, Gogoi N, Gahtori P, Singh N, Bhattacharyya DR, Singh UP, Bhat HR
Reference: 
J Biochem Mol Toxicol. 2020 Dec 17:e22682

Malaria continues to become a major global health problem, particularly in Sub-Saharan Africa, Asia, and Latin America. The widespread emergence of resistance to first-line drugs has further bolstered an urgent need for a new and cost-effective antimalarial(s). Thus, the present study enumerates the synthesis of novel hybrid dimethoxy pyrazole 1,3,5-triazine derivatives 7(a-j) and their in silico results short-listed three compounds with good binding energies and dock scores.

NOT Open Access | Ligand Decorated Primaquine loaded Nanocarriers for Liver Targeting for Triggered Antimalarial Activity

December 3, 2020 - 12:56 -- NOT Open Access
Author(s): 
Paramjot Mehan, Ashish Garg, Kumar Ajay, Neeraj Mishra
Reference: 
Curr Mol Pharmacol. 2020 Nov 25

The aim of the current research to formulate a nano delivery system for effective delivery of primaquine for liver targeting to achieve the potential antimalarial activity. An objective of current development is to formulate a lactobionic acid conjugated polyphosphazene based nanodelivery of primaquine for liver targeting to distinguish antimalarial activity.

Evaluation of a single screen and treat strategy to detect asymptomatic malaria among pregnant women from selected health facilities in Lindi region, Tanzania

December 2, 2020 - 09:45 -- Open Access
Author(s): 
Chonge Kitojo, Frank Chacky, Emmanuel S. Kigadye, Joseph P. Mugasa, Abdallah Lusasi, Ally Mohamed, Patrick Walker, Erik J. Reaves, Julie R. Gutman & Deus S. Ishengoma
Reference: 
Malar J 19, 438 (2020)

In areas of high transmission, malaria in pregnancy (MiP) primarily causes asymptomatic infections; these infections nonetheless increase the risk of adverse maternal and fetal outcomes. In 2014, Tanzania initiated a single screening and treatment (SST) strategy for all pregnant women at their first antenatal care (ANC) visit using malaria rapid diagnostic tests (RDT) for surveillance purposes. However, there is paucity of data on the effectiveness of SST in the prevention of MiP. The objective of this study was to estimate the number of asymptomatic infections among pregnant women detected by SST, which would have been missed in the absence of the policy.

NOT Open Access | Antimalarial activity of tetrahydro-beta-carbolines targeting the ATP binding pocket of the Plasmodium falciparum heat shock 90 protein

November 4, 2020 - 16:01 -- NOT Open Access
Author(s): 
Eagon S, Hammill JT, Kiplin Guy R, et al.
Reference: 
Bioorg Med Chem Lett. 2020 Nov 1;30(21):127502

A series of tetrahydro-β-carboline derivatives of a lead compound known to target the heat shock 90 protein of Plasmodium falciparum were synthesized and assayed for both potency against the parasite and toxicity against a human cell line.

Doxycycline has distinct apicoplast-specific mechanisms of antimalarial activity

November 4, 2020 - 14:34 -- Open Access
Author(s): 
Okada M, Guo P, Nalder SA, Sigala PA
Reference: 
Elife. 2020 Nov 2;9:e60246

Doxycycline (DOX) is a key antimalarial drug thought to kill Plasmodium parasites by blocking protein translation in the essential apicoplast organelle. Clinical use is primarily limited to prophylaxis due to delayed second-cycle parasite death at 1-3 µM serum concentrations. DOX concentrations >5 µM kill parasites with first-cycle activity but have been ascribed to off-target mechanisms outside the apicoplast.

Retargeting azithromycin analogues to have dual-modality antimalarial activity

October 1, 2020 - 15:25 -- Open Access
Author(s): 
Burns AL, Sleebs BE, Wilson DW, et al.
Reference: 
BMC Biol. 2020 Sep 29;18(1):133

Resistance to front-line antimalarials (artemisinin combination therapies) is spreading, and development of new drug treatment strategies to rapidly kill Plasmodium spp. malaria parasites is urgently needed. Azithromycin is a clinically used macrolide antibiotic proposed as a partner drug for combination therapy in malaria, which has also been tested as monotherapy. However, its slow-killing ‘delayed-death’ activity against the parasite’s apicoplast organelle and suboptimal activity as monotherapy limit its application as a potential malaria treatment. Here, we explore a panel of azithromycin analogues and demonstrate that chemical modifications can be used to greatly improve the speed and potency of antimalarial action.

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