antileishmanial agent1

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

Antileishmanial agent-10 (Compound 7h) is an antiprotozoal agent effective against leishmaniasis.

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-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-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-17, a coumarin hybrid, exhibits potent antileishmanial activity (IC50 <0.78 μM) while proving non-toxic to normal VERO cells. It specifically interacts with the folate pathway enzymes pteridine reductase and DHFR-TS. Efficacy against the promastigote form is highlighted by an IC50 value of 0.40 μM, and against the amastigote form, an IC50 of 0.68 μM, respectively.

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