antileishmanial

Antileishmanial agent-25 (compound 24) exhibits selective activity against intracellular amastigotes, demonstrating an inhibitory concentration (IC50) of 6.63 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-24 (compound 33) exhibits antileishmanial activity, demonstrating an inhibitory concentration 50 (IC50) value of 5.39 μM against amastigotes [1].

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

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

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

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

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-7 (compound 23) exhibits strong antileishmanial activity against Leishmania donovani and L-6, with IC50 values of 6.89 and 259 μM, respectively [1].

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

Antileishmanial agent-22 (compound 15b) serves as an antiparasitic and antibacterial, exhibiting activities against Leishmania (IC50 = 0.408 μM), malaria, and tuberculosis. It operates on an antifolate mechanism, suppressing both folic and folinic acids with 88% and 94% efficacy at 100 μM, respectively. This compound also demonstrates a 96.67% inhibitory effect on P. berghei 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-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-8 (compound 18) shows potent and selective activity against Leishmania donovani ( L. donovani ) (IC50 = 5.64 μM) with relatively low cytotoxicity in L-6 cells (IC 50 =73.9 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) exhibits potent activity against L. major promastigotes and amastigotes, demonstrating IC50 values of 0.78 μM for promastigotes and 0.99 μM for amastigotes, while also showing cytotoxicity at these concentrations [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-12 (compound 5a) is a potent anti-leishmanial agent with antibacterial activity against Leishmania brazilensis (IC50: 14.9 μM), Leishmania infantum (IC50: 21.3 μM) and T. cruzi (IC50. 9.3 μM). 9.3 μM) had antiprotozoal effects.

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-4 is a ribonucleoside analogue with potent activity against L.infantum and T.cruzi, having EC 50 values of 0.68 μM and 0.83 μM, respectively [1].

Antileishmanial agent-2 is a 3-Br-isoxazoline-Based Inhibitors against Plasmodium falciparum (D10 and W2 strains) and Leishmania spp. (L. infantum and L. tropica) Promastigotes with IC50s of 0.035, 0.058, 3.5 and 7.5 μM.

Topoisomerase I Inhibitor 9 (compound 3d), a specific inhibitor of leishmanial topoisomerase IB, exhibits antileishmanial activity, demonstrating an IC50 value of 34.81μM against L. donovani promastigotes [1].

Lysicamine shows significant antioxidant capacity in the ORAC(FL) assay and it is active against S. epidermidis and C. dubliniensis, with MIC values in the range 12.5-100 microg mL(-1). Lysicamine has antimicrobial and anti-inflammation activity, the mini

1. β-Hederin has antileishmanial activity. 2. β-Hederin has apoptotic effect on breast cancer cells, it could be a promising candidate for chemotherapy of breast cancer.

Amphotericin B trihydrate, a polyene antibiotic, is derived from Streptomyces nodosus fermenter cultures. It exhibits antileishmanial properties.

FD-838 shows good antileishmanial and moderate anticancer activities, it can moderately inhibit the growth of cultured P388 and HL-60 cell lines. FD-838 has anti-fungal activity, it can significantly inhibit the growth of two plant fungal pathogens Botryt

Compound 13, a topoisomerase I inhibitor 10, selectively inhibits leishmanial topoisomerase IB and exhibits antileishmanial activity. Specifically, it demonstrates efficacy against L. donovani promastigotes with an IC50 value of 27.91 μM [1].

Grifolin has anti-cancer effects, it induces apoptosis and promotes cell cycle arrest in the A2780 human ovarian cancer cell line via inactivation of the ERK1/2 and Akt pathways; it enhances the differentiation and proliferation of oligodendrocyte precurs

14-Norpseurotin A shows good antileishmanial and moderate anticancer activities. It also displays significant antimicrobial activities against Escherichia coli, Bacillus subtilis, and Micrococcus lysoleikticus with MICs of 3.74, 14.97, and 7.49 microM , r

Niazinin shows antileishmanial activity against promastigotes of Leishmania donavani, with an IC50 value of 5.25 microM.

Isopimpinellin (4,9-Dimethoxypsoralen) is a natural product isolated from the roots of Pimpinella saxifrage with antiviral and antileishmanial activity.

N-(2-Hydroxypropyl)methacrylamide is used in the synthesis of copolymers for the targeted delivery of antileishmanial agents in Visceral leishmaniasis.

HYPOCRELLIN B are photosensitive pigments isolated from Hypocrella bambusae Sacc. Hypocrellin B causes DNA strand breakage, induces apoptosis in ovarian cancer cells, and inhibits proliferation of Staphylococcus by increasing ROS levels, and damaging cell

Valeranone shows antileishmanial and cytotoxic activity.

Ludaconitine, isolated from Aconitum spicatum (Bruhl) Stapf, exhibits antileishmanial activity with an IC50 of 36.10 μg/mL.

Veraguensin is derived from Magnolia sp.. Veraguensin inhibits bone resorption and shows high antileishmanial activity.

Phylloflavan, an antileishmanial compound, exhibits an intracellular half maximal effective concentration (EC50) of 3.2 nM in RAW 264.7 cells and inhibits the cytopathic effect of encephalomyocarditis virus on L929 fibroblast cells at 38 units per milliliter (U/mL) [1].

DNDI-8219 is an antitubercular agent. It has potent antileishmanial effects.

Camaric acid shows antibacterial activity against Staphylococcus aureus and methicillin resistant S. aureus with IC50 values 8.74 and 8.09 uM, respectively, it also shows moderate antileishmanial activity and highly potent antitrypanosomal activity. Camar

3,5-Dihydroxybenzaldehyde is a building block.1,2It has been used in the synthesis of 2,4-dimethylbenzoylhydrazones with antileishmanial and antioxidant activities. 1.Taha, M., Baharudin, M.S., Ismail, N.H., et al.Synthesis of 2-methoxybenzoylhydrazone and evaluation of their antileishmanial activityBioorg. Med. Chem. Lett.23(11)3463-3466(2013) 2.Taha, M., Ismail, N.H., Jamil, W., et al.Synthesis, evaluation of antioxidant activity and crystal structure of 2,4-dimethylbenzoylhydrazonesMolecules18(9)10912-10929(2013)

Cabotegravir sodium is a potent inhibitor of HIV integrase and is able to act on HIVADA (IC50: 2.5 nM). cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1 and is less likely to interact with other antiretroviral drugs (ARVs). Antileishmanial agent-12

Pancixanthone A may have antimalarial activity, it also shows a significant antileishmanial activity against the promastigote forms of Leishmania mexicana and L. infantum and against the amastigote forms of L. infantum.

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)

Persicogenin has anticancer, antimutagenic, and antileishmanial activities, it can inhibit the proliferation of mouse tsFT210 cancer cells, it mainly inhibits cell cycle at the G2/M phase in a dose-dependent manner.

ICA (N-[4-(2-Pyridinyl)-2-thiazolyl]-2-pyridinamine) is a SK channel inhibitor and exhibits antileishmanial activity (IC50: 2.1 µM).

Euphorbadienol is a triterpenic compound isolated from the latex of Euphorbia resinifera. It has antileishmanial and antitrypanosomal activity.

Rohitukine is an anti-cancer agent. It modulates apoptosis pathways through gastrin antagonism and H(+) K (+)-ATPase inhibition. Rohitukine ia an antiadipogenic, antidyslipidemic, gastroprotective, antifertility, and antileishmanial compound.