antimalarial agent-1

Antimalarial agent 1 is an effective antimalarial agent.

Antimalarial agent 14 (NSC-102533) is a bioactive chemical.

Antimalarial agent 13 (N2-(3-chlorophenyl)-N4-(furan-2-ylmethyl)quinazoline-2,4-diamine) is a potent antimalarial agent.

Antimalarial agent 11 (compound 1), a spirocyclic chromane, is a potent antimalarial agent effective against D6 (EC50: 1.48 μM) and ARC08-022 (EC50: 1.81 μM).

Antimalarial agent 17 is an effective antimalarial agent and herbicide, also a photosystem II inhibitor with post-emergence herbicidal activity.

Antimalarial agent 19 (compound 6e) exhibits antimalarial activity against the blood stages of P. falciparum K1 and P. berghei, with EC50 values of 0.3 µM and 15.3 µM, respectively. It demonstrates good aqueous solubility, intestinal permeability, and microsomal stability relative to gamhepathiopine [1].

Antimalarial agent 10 (Compound 17b) is an amino alcohol-quinoline compound. It exhibits antimalarial activity against Pf3D7 (IC50: 14.9 nM) and PfW2 (IC50: 11 nM) with a selectivity index greater than 770, irrespective of the cell line.

Antimalarial agent 15 is a parasite inhibitor that exhibits antimalarial effects and inhibits the growth of Plasmodium falciparum 3D7 with an IC50 value of 20 nM.

Antimalarial agent 12 is an effective antimalarial agent that inhibits the growth of Plasmodium falciparum strains Dd2 and 3D7 with EC50 values of 155 nM and 136 nM, respectively. antimalarial agent 12 has a MIC >250,000 nM against E. coli and also acts on Antimalarial agent 12 has a MIC of >250,000 nM against E. coli and also works on HEK-293 and hPHep cell lines with CC50 values of 10,000-50,000 nM.

Antimalarial agent 16 is a parasite inhibitor that exhibits antimalarial effects and inhibits the growth of Plasmodium falciparum with an IC50 value of 2.0 nM.

Antimalarial agent 18, a powerful antimalarial compound characterized by its electronic, highly lipophilic, and siderophoric properties, falls within the acyloxymethyl series, acting as a fosmidomycin surrogate. It effectively inhibits the non-mevalonate isoprenoid biosynthesis pathway by targeting the IspC enzyme. This compound demonstrates significant inhibitory activity against P. falciparum (IC50 = 50 nM) and A. baumanii (IC50 = 390 nM).

Mefloquine (Ro 215998), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus, and cancer research.

MMV665916 is a quinazolinedione derivative that is an antimalarial agent. MMV665916 shows remarkable antiplasmodial activity against P. falciparum FcB1 strain with EC 50 value of 0.4 μM and presents the high selectivity index (SI>250) [1].

Emoquine-1 is a potent orally active antimalarial agent effective against various drug-resistant Plasmodium strains, including artemisinin-resistant dormant parasites. It demonstrates efficacy against proliferative malignant Plasmodium with an IC50 value ranging from 20 to 55 nM. Emoquine-1 holds potential for treating Plasmodium strains resistant to artemisinin combination therapy (ACT), with the capability to eradicate persistent parasites.

Insecticidal agent 19 (Compound 7b) exhibits antimalarial activity by inhibiting dihydrofolate reductase-thymidylate synthase (DHFR-TS) and pteridine reductase 1 (PTR1) through the folate metabolic pathway. This compound also inhibits the promastigote and amastigote forms of Leishmania major, with IC50 values of 1.43 μM and 3.78 μM, respectively.

PfThrRS-IN-1 (compound 11) is a potent inhibitor of the Plasmodium falciparum threonyl-tRNA synthetase (PfThrRS), exhibiting an IC50 value of 0.1 μM. This compound is also an effective antimalarial (antimalaria) agent.

FR900098 is an antimalarial agent that inhibits 1-deoxy-D-xylulose-5-phosphate (DXP) reductoisomerase. It exhibits no significant acute toxicity or genotoxicity and does not have the capability to cause chromosomal breaks or heterogeneity. Additionally, FR900098 has no impact on the bone marrow erythrocytes of NMRI mice.

Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a member of the 4-aminoquinoline class, is an antimalarial agent that also acts as a potent oral histamine N-methyltransferase inhibitor with a K i value of 18.6 nM. Additionally, it functions as a Nurr1 agonist, targeting the Nurr1-LBD (ligand binding domain) with an EC 50 of approximately 20 μM, demonstrating anti-inflammatory effects [1] [2] [3] [4] [5].

HLI373 dihydrochloride is a potent Hdm2 inhibitor, efficiently restraining the ubiquitin ligase activity of Hdm2 and effectively prompting apoptosis in DNA-damaging agent-sensitive tumor cells[1]. Additionally, HLI373 dihydrochloride exhibits antimalarial activity[2].

JMI-105 has the potential as an antimalarial agent. JMI-105 is a potent inhibitor of Plasmodium falciparum falcipain-2 protease (PfFP-2) that inhibits the P. falciparum strains CQ S (3D7) and CQ R (RKL-9) growth with IC 50 values of 8.8 μM and 14.3 μM. In a murine model with P. berghei ANKA infection, JMI-105 significantly decreases parasitemia and prolonged host survival [1].

Piperaquine tetraphosphate, a potent antimalarial agent, demonstrates inhibitory effects against both chloroquine-sensitive and chloroquine-resistant malaria isolates. When combined with dihydroartemisinin, it holds potential for researching chloroquine-resistant malaria [1] [2].

Hydroxychloroquine Impurity F, an impurity in Hydroxychloroquine, is identified in the synthetic antimalarial agent known for its capability to inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Additionally, Hydroxychloroquine demonstrates effective inhibition of SARS-CoV-2 infection in vitro [1] [2] [3].

Antimalarial agent 23, a benzimidazole-based compound, exhibits potent antimalarial activity, demonstrated by its low IC50 values of 0.08 μM for PfNF54 and 0.10 μM for PfK1, respectively. This compound effectively inhibits β-hematin formation, yet it does not directly interfere with the conversion of heme to hemozoin [1].

Quinine hemisulfate hydrate is an alkaloid extracted from the bark of cinchona, which has antimalarial effect. Quinine hemisulfate hydrate can be used as a potassium ion channel inhibitor to inhibit the voltage-induced mSlo3(KCa5.1) channel current, and its IC₅₀ is 169 μM under the condition of +100 mV.