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NOT Open Access | Microwave-assisted synthesis of hybrid PABA-1,3,5-triazine derivatives as an antimalarial agent

July 28, 2021 - 14:09 -- NOT Open Access
Kashyap A, Choudhury AAK, Saha A, Adhikari N, Ghosh SK, Shakya A, Patgiri SJ, Bhattacharyya DR, Singh UP, Bhat HR
J Biochem Mol Toxicol. 2021 Jul 27:e22860

The present manuscript deals with the development of novel p-aminobenzoic acid (PABA) associated 1,3,5-triazine derivatives as antimalarial agents. The molecules were developed via microwave-assisted synthesis and structures of compounds were ascertained via numerous analytical and spectroscopic techniques. The synthesized compounds were also subjected to ADMET analysis.

NOT Open Access | Chloroquine inhibits pro-inflammatory effects of heme on macrophages and invivo

July 28, 2021 - 14:06 -- NOT Open Access
Silva RCMC, Tan L, Rodrigues DA, Prestes EB, Gomes CP, Gama AM, Oliveira PL, Paiva CN, Manoury B, Bozza MT
Free Radic Biol Med. 2021 Jul 22;173:104-116

Chloroquine has been used successfully to treat Malaria, including by chloroquine-resistant Plasmodium sp., indicating that it has effects on disease itself. Since heme has inflammatory effects and contributes to the pathogenesis of hemolytic diseases, we hypothesize that the anti-inflammatory effect of chloroquine is partially due to its inhibitory effect on heme-induced macrophage activation and on inflammatory tissue damage.

Effect of α-tocopheryloxy acetic acid, a vitamin E derivative mitocan, on the experimental infection of mice with Plasmodium yoelii

June 30, 2021 - 12:17 -- Open Access
Kasumi Kawamura, Aiko Kume, Rika Umemiya-Shirafuji, Shunji Kasai and Hiroshi Suzuki
Malaria Journal 2021 20:280, 24 June 2021

Malaria parasites are known to be vulnerable to oxidative stress. In this study, the effects of the administration of α-tocopheryloxy acetic acid (α-TEA), which is a vitamin E analogue mitocan, on Plasmodium yoelii infection in mice were examined.

Interactions of primaquine and chloroquine with PEGylated phosphatidylcholine liposomes

June 16, 2021 - 15:09 -- Open Access
Miatmoko A, Nurjannah I, Nehru NF, Rosita N, Hendradi E, Sari R, Ekowati J
Sci Rep. 2021 Jun 14;11(1):12420

This study aimed to analyze the interaction of primaquine (PQ), chloroquine (CQ), and liposomes to support the design of optimal liposomal delivery for hepatic stage malaria infectious disease. The liposomes were composed of hydrogenated soybean phosphatidylcholine, cholesterol, and distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy[polyethyleneglycol]-2000), prepared by thin film method, then evaluated for physicochemical and spectrospic characteristics. The calcein release was further evaluated to determine the effect of drug co-loading on liposomal membrane integrity.

Not Open Access | Safety of treatment with chloroquine and hydroxychloroquine: A ten-year systematic review and meta-analysis

June 1, 2021 - 12:41 -- NOT Open Access
Edington FLB, Gadellha SR, Santiago MB
Eur J Intern Med. 2021 Jun;88:63-72

To estimate the incidence rate ratio (IRR) of adverse events (AE) in chloroquine or hydroxychloroquine users.

NOT Open Access | High proportion of genome-wide homology and increased pre-treatment pvcrt levels in Plasmodium vivax late recurrences: a chloroquine therapeutic efficacy study

May 26, 2021 - 09:40 -- NOT Open Access
Rovira-Vallbona E, Van Hong N, Rosanas-Urgell A, et al.
Antimicrob Agents Chemother. 2021 May 24:AAC.00095-21

Chloroquine (CQ) is the first-line treatment for Plasmodium vivax malaria in most endemic countries. Monitoring P.vivax CQ resistance (CQR) is critical but remains challenged by the difficulty to distinguish real treatment failure from reinfection or liver relapse. Therapeutic efficacy of CQ against uncomplicated P.vivax malaria was evaluated in Gia Lai province, Vietnam. Sixty-seven patients were enrolled and followed-up for 42 days using microscopy and (RT)qPCR.

NOT Open Access | Phytol suppresses parasitemia and ameliorates anaemia and oxidative brain damage in mice infected with Plasmodium berghei

May 5, 2021 - 11:01 -- NOT Open Access
Usman MA, Usman FI, Abubakar MS, Salman AA, Adamu A, Ibrahim MA
Exp Parasitol. 2021 May;224:108097

The quest for the development of a novel antimalarial drug informed the decision to subject phytol to in vivo trials following a demonstration of therapeutic potential against chloroquine sensitive strain of Plasmodium falciparum under in vitro condition. On this basis, the in vivo anti-Plasmodium berghei activity of phytol including the ameliorative effects of the compound on P. berghei-associated anaemia and organ damage were investigated.

NOT Open Access | Treatment with chloroquine is retinotoxic in captive African penguins (Speniscus demersus). Attenuation and recovery of electroretinographic responses

April 28, 2021 - 14:05 -- NOT Open Access
Ross M, Avni-Magen N, Pe'er O, Berkowitz A, Ofri R
Vet Ophthalmol. 2021 Apr 26

To evaluate the effect of prophylactic anti‐malarial chloroquine treatment, and its cessation, on electroretinographic (ERG) responses of captive African penguins.

Chloroquine: Autophagy inhibitor, antimalarial, bitter taste receptor agonist in fight against COVID-19, a reality check

April 22, 2021 - 08:29 -- Open Access
Sharma P, McAlinden KD, Ghavami S, Deshpande DA
Eur J Pharmacol. 2021 Apr 15;897:173928

The recent SARS-CoV-2 pandemic poses one of the greatest challenges to modern medicine. Therefore, identification of new therapeutic strategies seems essential either based on novel vaccines or drugs or simply repurposing existing drugs. Notably, due to their known safety profile, repurposing of existing drugs is the fastest and highly efficient approach to bring a therapeutic to a clinic for any new indication. One such drug that has been used extensively for decades is chloroquine (CQ, with its derivatives) either for malaria, lupus and rheumatoid arthritis.

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).


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