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antiplasmodial Agent

NOT Open Access | Design, synthesis and biological evaluation of mono- and bisquinoline methanamine derivatives as potential antiplasmodial agents

April 20, 2021 - 15:27 -- NOT Open Access
Bokosi FRB, Beteck RM, Mbaba M, Mtshare TE, Laming D, Hoppe HC, Khanye SD
Bioorg Med Chem Lett. 2021 Apr 15;38:127855

Several classes of antimalarial drugs are currently available, although issues of toxicity and the emergence of drug resistant malaria parasites have reduced their overall therapeutic efficiency. Quinoline based antiplasmodial drugs have unequivocally been long-established and continue to inspire the design of new antimalarial agents. Herein, a series of mono- and bisquinoline methanamine derivatives were synthesised through sequential steps; Vilsmeier-Haack, reductive amination, and nucleophilic substitution, and obtained in low to excellent yields.

NOT Open Access | Synthesis and biological evaluation of benzhydryl-based antiplasmodial agents possessing Plasmodium falciparum chloroquine resistance transporter (PfCRT) inhibitory activity

April 6, 2021 - 14:20 -- NOT Open Access
Relitti N, Federico S, Pozzetti L, Campiani G, et al.
Eur J Med Chem. 2021 Apr 5;215:113227

Due to the surge in resistance to common therapies, malaria remains a significant concern to human health worldwide. In chloroquine (CQ)-resistant (CQ-R) strains of Plasmodium falciparum, CQ and related drugs are effluxed from the parasite's digestive vacuole (DV). This process is mediated by mutant isoforms of a protein called CQ resistance transporter (PfCRT). CQ-R strains can be partially re-sensitized to CQ by verapamil (VP), primaquine (PQ) and other compounds, and this has been shown to be due to the ability of these molecules to inhibit drug transport via PfCRT.

NOT Open Access | 3-aryl-indolinones derivatives as antiplasmodial agents: synthesis, biological activity and computational analysis

March 17, 2021 - 09:06 -- NOT Open Access
Luczywo A, González LG, Mellado M, et al.
Nat Prod Res. 2021 Mar 11:1-7

Malaria is an infectious illness, affecting vulnerable populations in Third World countries. Inspired by natural products, indole alkaloids have been used as a nucleus to design new antimalarial drugs. So, eighteen oxindole derivatives, aza analogues were obtained with moderate to excellent yields. Also, the saturated derivatives of oxindole and aza derivatives via H2/Pd/C reduction were obtained in good yields, leading to racemic mixtures of each compound.

NOT Open Access | 3-Hydroxy-propanamidines, a New Class of Orally Active Antimalarials Targeting Plasmodium falciparum

March 9, 2021 - 15:29 -- NOT Open Access
Knaab TC, Held J, Kurz T, et al.
J Med Chem. 2021 Mar 5

3-Hydroxypropanamidines are a new promising class of highly active antiplasmodial agents. The most active compound 22 exhibited excellent antiplasmodial in vitro activity with nanomolar inhibition of chloroquine-sensitive and multidrug-resistant parasite strains of Plasmodium falciparum (with IC50 values of 5 and 12 nM against 3D7 and Dd2 strains, respectively) as well as low cytotoxicity in human cells.

NOT Open Access | Toward a Stable and Potent Coenzyme A-Targeting Antiplasmodial Agent: Structure-Activity Relationship Studies of N-Phenethyl-α-methyl-pantothenamide

July 15, 2020 - 14:32 -- NOT Open Access
Spry C, Barnard L, Kok M, Powell AK, Mahesh D, Tjhin ET, Saliba KJ, Strauss E, de Villiers M
ACS Infect Dis. 2020 Jul 10;6(7):1844-1854

Pantothenamides (PanAms) are potent antiplasmodials with low human toxicity currently being investigated as antimalarials with a novel mode of action. These structural analogues of pantothenate, the vitamin precursor of the essential cofactor coenzyme A, are susceptible to degradation by pantetheinase enzymes present in serum. We previously discovered that α-methylation of the β-alanine moiety of PanAms increases their stability in serum and identified N-phenethyl-α-methyl-pantothenamide as a pantetheinase-resistant PanAm with potent, on-target, and selective antiplasmodial activity.

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