leishmaniasis

Dapsone (Sulphadione) has activity against a wide range of bacteria but mainly employed for its actions against mycobacterium leprae.

Paromomycin binds specifically to the RNA oligonucleotide at the A site of bacterial 30S ribosomes, thereby causing misreading and premature termination of translation of mRNA and inhibition of protein synthesis followed by cell death. Paromomycin Sulfate (Aminosidine sulfate) is the sulfate salt form of paromomycin, a structural derivative of neomycin, an aminoglycoside antibiotic with amebicidal and bactericidal effects against predominantly aerobic gram-negative bacteria.

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

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin also exhibits anti-hepatitis B virus, antiinflammatory and antiallodynic actions.

DNDI-6148 has anti-experimental cutaneous leishmaniasis activity and can be used to study visceral leishmaniasis by inhibiting Leishmania protozoa cleavage and polyadenylation-specific factor (CPSF3) endonuclease.

GSK3494245 is a Leishmania donovani inhibitor that suppresses trypsin-like activity catalyzed by the β5 subunit of L. donovani proteasome, applicable for visceral leishmaniasis (VL) studies.

Miltefosine (HePC) is the treatment of visceral and cutaneous leishmaniasis drug , and is proceeding clinical trials for this in several countries. Several medical agents produce some potency against visceral or cutaneous leishmaniasis, however a 2005 survey concluded that miltefosine is the only effective oral treatment for both forms of leishmaniasis.

Acivicin (AT-125), a chlorinated amino acid antibiotic produced by Streptomyces porcineus, is a γ-glutamyl transpeptidase (GGT) inhibitor that crosses the blood-brain barrier, exhibits anticancer and antiparasitic activity, and is used in the study of visceral leishmaniasis.

PK 11195 (RP 52028) is a TSPO ligand for neuroimaging that exhibits significant protection against CoCl2-induced alterations and can be used to study leishmaniasis.

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.

DHODH-IN-29 (Compound 2i) is a covalent inhibitor of Leishmania braziliensis dihydroorotate dehydrogenase (LbDHODH), with an IC50 value of 0.5 μM. It shows potential for use in leishmaniasis research.

Antiparasitic agent-27 (Compound 2) is a potent antiparasitic compound targeting Leishmania infantum with an IC50 of 3.1 μM. It induces cell cycle arrest in the G0/G1 phase and enhances reactive oxygen species (ROS) production to trigger programmed cell death, showing promise for visceral leishmaniasis (VL) research.

Antileishmanial agent-35 (Compound 6) is an antileishmanial compound with an IC50 of 0.29 μM against the promastigotes of Leishmania amazonensis. It acts by disrupting the electron transport chain (where ubiquinone plays a role), markedly reducing mitochondrial membrane potential and ATP levels, and increasing reactive oxygen species (ROS) production. Antileishmanial agent-35 is applicable in the study of cutaneous leishmaniasis.

DNDI-0690 is a potent and orally active analogue of DNDI-VL-2098, demonstrating significant efficacy against cutaneous leishmaniasis (CL). It exhibits notable in vitro activity against Leishmania parasites responsible for CL, with an EC50 of 0.17 μM for visceral leishmaniasis and an EC50 of less than 5 μM for the causative parasites of CL. Additionally, DNDI-0690 is effective in a L. major CL mouse model and is applicable for research in CL.

Antileishmanial agent-38 (compound 197) is a host-targeted small molecule exhibiting potent broad-spectrum activity against Leishmania spp. This compound primarily works by targeting host protein lysozyme to inhibit intracellular parasites and also shows direct activity against extracellular L. donovani promastigotes. Antileishmanial agent-38 is applicable in leishmaniasis research.

1,4-Dihydrazinylphthalazine (Compound 2) is an antiparasitic agent targeting Leishmania spp. It shows potential for use in tropical disease research, particularly in studying cutaneous leishmaniasis.

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally bioavailable, selective, and allosteric inhibitor of Akt with an IC50 of 2.7 nM, 14 nM, and 8.1 nM against Akt1, Akt2, and Akt3, respectively. It also shows significant potency against the AKT1-E17K mutant protein and holds promise for research on PI3K/AKT-driven tumors and Proteus syndrome. Additionally, Miransertib hydrochloride exhibits efficacy against Leishmania [1, 2].

Benzoxonium chloride, The topical treatment of anthroponotic cutaneous leishmaniasis with the tincture of thioxolone plus benzoxonium chloride (Thio-Ben) along with cryotherapy.

Aminoquinol diphosphate may be useful in the treatment of acute necrotising cutaneous leishmaniasis.

Aminoquinol triphosphate may be useful in the treatment of acute necrotising cutaneous leishmaniasis.

LXE408 is an orally active, kinetoplastid-selective proteasome inhibitor, exhibiting non-competitive inhibitory effects. It demonstrates an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Moreover, LXE408 shows limited ability to traverse the blood-brain barrier. Hence, LXE408 holds promise for advancing research in the field of visceral leishmaniasis (VL).

LXE408 fumarate is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 fumarate has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 fumarate has a low propensity to cross the blood brain barrier. LXE408 fumarate has the potential for visceral leishmaniasis (VL) research.

PT4 is a treatment agent for Cutaneous leishmaniasis (CL). PT4 decreases of mitochondrial membrane potential and increases reactive oxygen species production, therefore leads to parasite death. PT4 is effective against both species of Leishmania. The IC50 values of PT4 against L. amazonensis and L. braziliensis are 125.18 and 233.18 μM , respectively. PT4 also shows potent anti-inflammatory activity in vivo [1].