gametocytes

MMV674850 exhibits potency against asexual stage parasites, with IC50 values of 2.7 and 4.5 nM. Furthermore, it demonstrates a preferential affinity for early-stage gametocytes, displaying an IC50 value of 4.5 ± 3.6 nM, compared to late-stage gametocytes with an IC50 value of 28.7 ± 0.2 nM.

Antimalarial agent 28 (Compound 2i) acts as an antiplasmodial agent, exhibiting inhibition of P. berghei with IC50 values of 0.561 μM for the liver stage, 0.14 μM for early gametocytes, and 4.34 μM for the ring stages of P. falciparum [1].

P-orlandin, a fungal metabolite, effectively impedes Plasmodium falciparum infection in mosquitoes by preventing FREP1 from binding to gametocytes or ookinetes [1].

MMV666810, a 2-aminopyrazine analogue of MMV390048, exhibits potent antiplasmodial activity against asexual parasites with an IC50 value of 5.94 nM. It demonstrates enhanced efficacy against late-stage gametocytes with a 3.3-fold higher selectivity relative to early stages (early-stage gametocyte: IC50 603 ± 88 nM; late-stage gametocyte: IC50 179 ± 8 nM).

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].

KDU691 is a PI4K inhibitor.