plasmodium

Atovaquone (Atavaquone) is a hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.

PfDHODH-IN-1, an analogue of the active Leflunomide metabolite, exhibits antimalarial activity.

SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).

Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A is a selective inhibitor of DNMT3B (IC50 = 500 nM).

KDU691 is a PI4K inhibitor.

Oxysanguinarine (Hydroxysanguinarine) possesses antiplatelet aggregation activity, it has potential inhibitory properties against the dengue virus.

13,21-Dihydroeurycomanone (Pasakbumin C) is a natural product isolated from the root of Eurycoma longifolia with antiparasitic activity such as Plasmodium falciparum and Toxoplasma gondii.

DHODH-IN-8 has antimalarial activity. DHODH-IN-8 is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC50 of 0.13 μM and 47.4 μM, and Kis of 0.016 μM and 5.6 μM, respectively.

FTI 276 TFA is effective against plasmodium falciparum and humans.It is a protein-based nikyltransferase (PFT) inhibitor with an IC50s of 0.9 nM and 0.5 nM, respectively.

Guanfu base H is a diterpenoid alkaloid isolated from Aconitum coreanum. It has antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (wild type) and K1CB1 (IC50s: 4 μM and 3.6 μM).

Isochondodendrine has strong antiplasmodial activity against Plasmodium falciparum. Isochondrodendrine is a class of bisbenzylisoquinoline alkaloid isolated from Isolona ghesquiereina.

L-Canaline, a nonprotein amino acid found in many leguminous plants, exhibits potent anticancer and antiproliferative effects. It effectively inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. Additionally, L-Canaline acts as a cytotoxic metabolite produced from L-canavanine through arginase catalysis and serves as a potent and irreversible inhibitor of ornithine aminotransferase.

MMV390048 is an antimalarial agent and is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 μM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns.

1. Tuberostemonine (Tuberstemonine) exhibits relatively higher intestinal permeabilities. 2. Tuberostemonine acts in part as an open-channel blocker at the crayfish neuromuscular junction.

PfDHODH-IN-2 is a dihydrothiophenone derivative, is a potent Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH, IC50 : 1.11 μM) inhibitor . It is used an antimalarial agent and can be used for the research of malaria

Cycloheximide (Naramycin A) is a natural product . Cycloheximide‘s IC50 values for protein synthesis and RNA synthesis in vivo are 532.5 nM and 2880 nM, respectively. Cycloheximide inhibits ferroptosis and autophagy and is an antifungal antibiotic.

Sporogen-AO 1, a compound from the commensal fungus Penicillium sp. G1-a14, is an inhibitor of human inducible nitric oxide synthase expression with antimalarial activity and strong cytotoxicity.

FNDR-20123 free base, a pioneering and orally administered anti-malarial agent, acts as a Histone Deacetylase (HDAC) inhibitor, displaying potent efficacy with IC50 values of 31 nM for Plasmodium and 3 nM for human HDAC, respectively. It effectively targets both the asexual (IC50=41 nM) and sexual blood stages (IC50=190 nM for male gametocytes) of Plasmodium falciparum. Additionally, FNDR-20123 free base inhibits multiple HDAC isoforms, namely HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with respective IC50 values of 25, 29, 2, 11, and 282 nM, and displays nanomolar inhibitory concentrations against Class III HDAC isoforms [1].

FNDR-20123 is the first safe and effective anti-malarial HDAC inhibitor, acting on both Plasmodium falciparum HDAC (IC50: 31 nM) and human HDAC (IC50: 3 nM). FNDR-20123 inhibited HDAC1 (IC50: 25 nM), HDAC2 (IC50: 29 nM), HDAC3 (IC50: 2 nM), HDAC6 (IC50: 11 nM), HDAC8 (IC50: 282 nM) and, at nanomolar concentrations, HDAC3 (IC50: 2 nM). The inhibitor of HDAC subtype III was also observed at nanomolar concentrations.

Artelinic acid is a water-soluble artemisinin analog with antimalarial activity and is used for the treatment of multi-drug resistant strains of Plasmodium falciparum.

CWHM-1552 is an effective Plasmodium falciparum inhibitor. For the 3D7 and Dd2 strains, the IC50s are 51 nM and 53 nM.

DHODH-IN-4 is a human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitor. The IC50 values of PfDHODH and HsDHODH are 4 μM and 0.18 μM, respectively. DHODH-IN-4 has antimalarial activity.

WR99210 hydrochloride is a potent inhibitor of Plasmodium falciparum dihydrofolate reductase (pfDHFR), which is a major malarial drug target. It has subnanomolar potency for the wild type, double mutant and quadruple mutant dihydrofolate reductases.

SNX0723 is a potent Hsp90 Inhibitor with anti-Plasmodium activity. SNX0723 shows high binding affinity for HsHsp90 and PfHsp90 with Kis of 4.4 and 47 nM, respectively. SNX0723 inhibits liver-stage P. berghei ANKA parasites with the EC50 of 3.3 μM.