leishmania

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

Leishmania peptide 183 is an antigen.

Compound 17k, also known as Antileishmanial agent-30, effectively inhibits Leishmania with an IC50 of 0.2 μM for L. donovani. It exhibits a CC50 of >100 μM and an SI of >500, indicating significant selectivity and potency.

Antileishmanial agent-26 (Compound 69) is a guanidine-containing compound with activity against *Leishmania donovani*, exhibiting an IC50 value of 5.67 μM and a CC50 value of 3.79 μM in THP-1 cells. This compound is applicable for research in tropical diseases.

Antileishmanial agent-27 (compound 7j) is a benzothiazole-coumarin derivative. It acts as a competitive inhibitor of arginyl-tRNA synthetase (ArgRS). This compound demonstrates selectivity towards the Leishmania donovani ArgRS (LdArgRS) over the human counterpart (HsArgRS), with IC50 values of 1.2 μM and 19 μM, respectively. Additionally, Antileishmanial agent-27 exhibits favorable pharmacokinetic properties.

Antileishmanial agent-29 (Compound 110) is an orally active compound that exhibits antileishmanial properties. It can protect mice from Leishmania infection when administered orally at doses of 40 or 60 mg/kg over a period of 10 days.

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-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-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-12 (compound 5a) is a potent antileishmanial agent with antibacterial activity against Leishmania braziliensis (IC50: 14.9 μM), Leishmania infantum (IC50: 21.3 μM), and T. cruzi (IC50: 9.3 μM), demonstrating significant antiprotozoal effects.

Antileishmanial agent-6 is a potent anti-leishmanial agent with anti-leishmanial activity (IC50: 0.54 μM) and cytotoxicity (IC50: 10.2 μM) against Leishmania donovani and L-6.

Antileishmanial agent-11 is a potent antileishmanial agent that acts on Leishmania brazilensis (IC50: 28.3 μM), Leishmania infantum (IC50: 24.8 μM) and T. cruzi (IC50: 13.0 μM) with outstanding antiprotozoal effect.

Antileishmanial agent-13, a quinoline-isatin hybrid, functions as an antileishmanial agent targeting the L. Major Leishmania strain through an anti-folate mechanism. This compound exhibits potent inhibition of both the promastigote and amastigote forms, boasting IC50 values of 0.604 μM and 0.508 μM, respectively.

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-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].

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-31 (Compound p1) is a pyrazole derivative exhibiting antileishmanial activity with an IC50 of 35.53 μg/mL. Furthermore, Antileishmanial agent-31 demonstrates high stability and is applicable in studies focused on leishmaniasis treatment.

Antileishmanial agent-33 (4e) is a hybrid compound of grandisin and machilin G, demonstrating moderate activity against promastigotes with an IC50 of 38.1 μM. In studies of cutaneous leishmaniasis (CL), Antileishmanial agent-33 (4e) has shown potential as an antileishmanial agent.

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