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NOT Open Access | In vitro and in vivo antiplasmodial activity of novel quinoline derivative compounds by molecular hybridization

April 6, 2021 - 13:54 -- NOT Open Access
Marinho JA, Martins Guimarães DS, Abramo C, et al.
Eur J Med Chem. 2021 Apr 5;215:113271

Chloroquine (CQ) has been the main treatment for malaria in regions where there are no resistant strains. Molecular hybridization techniques have been used as a tool in the search for new drugs and was implemented in the present study in an attempt to produce compound candidates to treat malarial infections by CQ-resistant strains. Two groups of molecules were produced from the 4-aminoquinoline ring in conjugation to hydrazones (HQ) and imines (IQ).

Repurposing of existing therapeutics to combat drug-resistant malaria

April 1, 2021 - 09:06 -- Open Access
Yadav K, Shivahare R, Shaham SH, Joshi P, Sharma A, Tripathi R
Biomed Pharmacother. 2021 Apr;136:111275

In the era of drug repurposing, speedy discovery of new therapeutic options for the drug-resistant malaria is the best available tactic to reduce the financial load and time in the drug discovery process. Six anticancer drugs, three immunomodulators and four antibiotics were selected for the repositioning against experimental malaria owing to their mode of action and published literature. The efficacy of existing therapeutics was evaluated against chloroquine-resistant in vitro and in vivo strains of Plasmodium falciparum and P. yoelii, respectively. All the pre-existing FDA-approved drugs along with leptin were primarily screened against chloroquine-resistant (PfK1) and drug-sensitive (Pf3D7) strains of P. falciparum using SYBR green-based antiplasmodial assay.

NOT Open Access | Antimalarial Quinacrine and Chloroquine Lose Their Activity by Decreasing Cationic Amphiphilic Structure with a Slight Decrease in pH

March 30, 2021 - 14:21 -- NOT Open Access
Kitagawa T, Matsumoto A, Terashima I, Uesono Y
J Med Chem. 2021 Mar 27

Quinacrine (QC) and chloroquine (CQ) have antimicrobial and antiviral activities as well as antimalarial activity, although the mechanisms remain unknown. QC increased the antimicrobial activity against yeast exponentially with a pH-dependent increase in the cationic amphiphilic drug (CAD) structure. CAD-QC localized in the yeast membranes and induced glucose starvation by noncompetitively inhibiting glucose uptake as antipsychotic chlorpromazine (CPZ) did.

Plasmodium vivax infection with exflagellated microgametes in peripheral blood smears

March 23, 2021 - 14:34 -- Open Access
Li THS, Lee ACH, Wong WS, Yip YL
Int J Infect Dis. 2021 Mar 18:S1201-9712(21)00267-8

A 42-year-old man with travel history to Qatar and India was admitted for feverish sensation, headache and epigastric discomfort. Peripheral blood smears showed intraerythrocytic parasites compatible with Plasmodium vivax [Fig. 1 (a) and (b)].

NOT Open Access | Does hydroxychloroquine still have any role in the COVID-19 pandemic

March 17, 2021 - 16:58 -- NOT Open Access
Schilling WH, White NJ
Expert Opin Pharmacother. 2021 Mar 16:1-10

The 4-aminoquinolines, chloroquine, and hydroxychloroquine have been used for over 70 years for malaria and rheumatological conditions, respectively. Their broad-spectrum antiviral activity, excellent safety profile, tolerability, low cost, and ready availability made them prime repurposing therapeutic candidates at the beginning of the COVID-19 pandemic.

Surveillance of Plasmodium falciparum pfcrt haplotypes in southwestern uganda by high‐resolution melt analysis

March 3, 2021 - 15:30 -- Open Access
Kennedy Kassaza, Anna C. Long, Yap Boum II, et al.
Malaria Journal 2021 20:114, 25 February 2021

Chloroquine (CQ) resistance is conferred by mutations in the Plasmodium falciparum CQ resistance transporter (pfcrt). Following CQ withdrawal for anti-malarial treatment, studies across malaria-endemic countries have shown a range of responses. In some areas, CQ sensitive parasites re-emerge, and in others, mutant haplotypes persist. Active surveillance of resistance mutations in clinical parasites is essential to inform treatment regimens; this effort requires fast, reliable, and cost-effective methods that work on a variety of sample types with reagents accessible in malaria-endemic countries.

Identification of Plasmodium falciparum heat shock 90 inhibitors via molecular docking

March 2, 2021 - 15:08 -- Open Access
Everson N, Bach J, Hammill JT, Falade MO, Rice AL, Guy RK, Eagon S
Bioorg Med Chem Lett. 2021 Mar 1;35:127818

A virtual screen was performed to identify anti-malarial compounds targeting Plasmodium falciparum heat shock 90 protein by applying a series of drug-like and commercial availability filters to compounds in the ZINC database, resulting in a virtual library of more than 13 million candidates. The goal of the virtual screen was to identify novel compounds which could serve as a starting point for the development of antimalarials with a mode of action different from anything currently used in the clinic.

NOT Open Access | Synthesis and antiplasmodial evaluation of 1H-1,2,3-triazole grafted 4-aminoquinoline-benzoxaborole hybrids and benzoxaborole analogues

February 25, 2021 - 10:13 -- NOT Open Access
Saini A, Kumar S, Raj R, Chowdhary S, Gendrot M, Mosnier J, Fonta I, Pradines B, Kumar V
Bioorg Chem. 2021 Feb 16;109:104733

A library of 1H-1,2,3-triazole-tethered 4-aminoquinoline-benzoxaborole hybrids as well as aryl substituted benzoxaborole analogues was synthesized and screened for their anti-plasmodial efficacy against both chloroquine-susceptibility 3D7 and chloroquine-resistant W2 strains of P. falciparum. The inclusion of quinoline core among the synthesized analogues resulted in substantial enhancement of anti-plasmodial activities.

NOT Open Access | A Novel Hybrid of Chloroquine and Primaquine Linked by Gold(I): Multitarget and Multiphase Antiplasmodial Agent

February 25, 2021 - 08:21 -- NOT Open Access
de Souza Pereira C, Costa Quadros H, Navarro M, et al.
ChemMedChem. 2021 Feb 17;16(4):662-678

Plasmodium parasites kill 435 000 people around the world every year due to unavailable vaccines, a limited arsenal of antimalarial drugs, delayed treatment, and the reduced clinical effectiveness of current practices caused by drug resistance. Therefore, there is an urgent need to discover and develop new antiplasmodial candidates. In this work, we present a novel strategy to develop a multitarget metallic hybrid antimalarial agent with possible dual efficacy in both sexual and asexual erythrocytic stages.

NOT Open Access | Distribution and temporal dynamics of P. falciparum chloroquine resistance transporter mutations associated with piperaquine resistance in Northern Cambodia

February 3, 2021 - 15:27 -- NOT Open Access
Shrestha B, Shah Z, Takala-Harrison S, et al.
J Infect Dis. 2021 Feb 2:jiab055

Newly emerged mutations within the Plasmodium falciparum chloroquine resistance transporter (PfCRT) can confer piperaquine resistance in the absence of amplified plasmepsin II (pfpm2). In this study, we estimated the prevalence of co-circulating piperaquine resistance mutations in P. falciparum isolates collected in northern Cambodia from 2009-2017.


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