antileishmanial agent 1

Antileishmanial agent-1 demonstrates activity against both L. amazonensis promastigotes (IC 50 = 15.52 μM) and intracellular amastigotes (IC 50 = 4.10 μM).

Sitamaquine is an antileishmanial agent.1It is active againstL. donovani,L. infantum,L. mexicana,L. braziliensis, andL. tropica(EC50s = 9.5-19.8 μM). It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH), in a cell-free assay when used at concentrations ranging from 10 to 200 μM.2Sitamaquine (100 μM) increases intracellular levels of reactive oxygen species (ROS) and decreases intracellular ATP levels, as well as induces phosphatidylserine externalization, chromatin fragmentation, and depolarization of the mitochondrial membrane potential, markers of apoptosis, inL. donovanipromastigotes. 1.López-Martín, C., Pérez-Victoria, J.M., Carvalho, L., et al.Sitamaquine sensitivity in Leishmania species is not mediated by drug accumulation in acidocalcisomesAntimicrob. Agents Chemother.52(11)4030-4036(2008) 2.Carvalho, L.J.M., Luque-Ortega, J.R., López-Martín, C., et al.The 8-aminoquinoline analogue sitamaquine causes oxidative stress in Leishmania donovani promastigotes by targeting succinate dehydrogenaseAntimicrob. Agents Chemother.55(9)4204-4210(2011)

Antileishmanial agent-8 (compound 18) exhibits potent and selective activity against Leishmania donovani (L. donovani) with an IC50 of 5.64 μM and relatively low cytotoxicity in L-6 cells with an IC50 of 73.9 μM [1].

Antileishmanial agent-4, a ribonucleoside analogue, functions as an antileishmanial agent [1].

Antileishmanial agent-3 (Compound 13) effectively inhibits the growth of *Leishmania major* [1].

Antileishmanial agent-9 (compound 16c) exhibits potent and selective activity against Leishmania donovani (L. donovani) with an IC50 value of 4.01 μM, while demonstrating relatively low cytotoxicity in L-6 cells with an IC50 value of 40.1 μM [1].

Antileishmanial agent-4 is a ribonucleoside analogue with potent activity against L. infantum and T. cruzi, exhibiting EC50 values of 0.68 μM and 0.83 μM, respectively [1].

Antileishmanial agent-7 (compound 23) exhibits potent antileishmanial activity against Leishmania donovani with an IC50 of 6.89 μM and against L-6 with an IC50 of 259 μM [1].

Antileishmanial agent-14, a sulfuretin analog, exhibits potential activity against Leishmania donovani promastigotes (IC 50 = 4.1 μM) and inhibits infection by L. donovani amastigotes (IC 50 = 11.1 μM) [1].

Antileishmanial agent-15 (compound 13c) demonstrates potent activity against L. major promastigotes and amastigotes with IC50 values of 0.78 μM and 0.99 μM, respectively, and exhibits cytotoxicity at these concentrations [1].

Antileishmanial agent-16 (compound 14c), an anti-Leishmania agent, exhibits potent activity against Leishmania major promastigotes (IC50 = 0.59 µM) and amastigotes (IC50 = 0.81 µM), while maintaining a favorable safety profile in mammalian cells (VERO cells) [1].

Antileishmanial agent-23 (compound G1 9), a potent and selective trypanothione reductase (TR) inhibitor, exhibits an IC50 of 2.24 ± 0.52 μM and effectively inhibits the growth of Leishmania, Trypanosoma cruzi, and Trypanosoma brucei [1].

Antileishmanial agent-24 (compound 33) exhibits antileishmanial activity with an inhibitory concentration 50 (IC50) value of 5.39 μM against amastigotes [1].

Compound F27 (Antileishmanial agent-19) is an antileishmanial compound effective against L. donovani promastigotes, demonstrating an IC50 of 3.39 μM. It functions by inhibiting the Leishmania prolyl-tRNA synthetase and disrupting the host PI3K Akt CREB axis-mediated IL-10 secretion. Additionally, Compound F27 promotes autophagy-mediated apoptosis in L. donovani promastigotes and has been shown to reduce parasite burden in L.d-infected animals [1].

Antileishmanial agent-20 exhibits selectivity against the Leishmania parasite, with IC50 values of 2.8 μM for L. infantum and 0.2 μM for L. braziliensis. It is a potential research tool for studying these parasites [1].

Antileishmanial agent-21 (compound 4e) functions as an inhibitor of Leishmania pteridine reductase 1 (Lm-PTR1), employing an anti-folate mechanism. Its antileishmanial effects can be negated by folic acid and leucovorin. Additionally, it demonstrates inhibitory activity against the chloroquine-resistant Plasmodium falciparum strain RKL9, with an IC50 ranging from 0.0198 to 0.096 μM [1].

Antileishmanial agent-22 (compound 15b) acts as an antiparasitic and antibacterial agent, demonstrating activity against Leishmania (IC50 = 0.408 μM), malaria, and tuberculosis. It functions via an antifolate mechanism, inhibiting folic and folinic acids with 88% and 94% efficacy at 100 μM. The compound inhibits P. berghei by 96.67% in vivo in vitro at 48.4 μM kg day and 0.038 μM (IC50), and it inhibits M. tuberculosis with an MIC of 28.44 μM [1].

Antileishmanial agent-25 (compound 24) exhibits selective activity against intracellular amastigotes with an inhibitory concentration (IC50) of 6.63 μM [1].

Antileishmanial agent-18 (Compound 1e) serves as an effective inhibitor of L. donovani promastigotes' growth, while maintaining safety for host cells [1].