Trypanosoma Inhibitor

PMX464 (AW 464) is a thiol-reactive quinol compound and an inhibitor of the thioredoxin-thioredoxin reductase (Trx/TrxR) system, with an IC₅₀ value of 6.5 μM against TrxR. PMX464 acts by irreversibly inhibiting the thioredoxin (Trx-1) system, blocking HIF-1α transcriptional activation and the NF-κB inflammatory pathway, inducing apoptosis, attenuating platelet function and inhibiting thrombosis, and specifically disrupting the trypanothione antioxidant metabolic network in parasites. PMX464 is used in research concerning malignant tumors (colorectal cancer, breast cancer, renal cancer, and leukemia), pulmonary inflammation, African sleeping sickness, and antithrombotic applications.

Antitrypanosomal agent 9 (compound 1) is a potent antitrypanosomal agent. Antitrypanosomal agent 9 shows inhibitory activity against T. b. brucei, with an IC₅₀ of 1.15 μM. Antitrypanosomal agent 9 can be used for human African trypanosomiasis (HAT) research.

Purine phosphoribosyltransferase-IN-2 is a potent inhibitor of the Plasmodium falciparum ((Pf)), Plasmodium vivax ((Pv)) and Trypanosoma brucei ((Tbr)) 6-oxopurine phosphoribosyltransferase (PRT), with K_is of 30, 20 and 2 nM, respectively.

Antitrypanosomal agent 10 is an antitrypanosomal agent that inhibits Trypanosoma cruzi with an IC₅₀ of 0.28 μM.

3β-Hydroxy-hop-22(29)-ene (compound 3) is a potent antiparasitic agent. 3β-Hydroxy-hop-22(29)-ene shows moderate activity against Trypanosoma cruzi and Leishmania mexicana.

Malonomicin (Antibiotic K16) is an antibiotic with anti-protozoa and anti-trypanosome activities. Malonomicin also shows anti-trypanosome activity in vivo.

Salviandulin E is a diterpenoid compound that can be isolated from Salvia leucantha CAV.. Salviandulin E shows antitrypanosomal activity against T. b. brucei GUTat 3.1 parasites with an IC₅₀ value of 0.72 µg/mL.

Anti-infective agent 5 (compound 74) is an orally active inhibitor of Trypanosoma cruzi with an IC₅₀ value of 0.10 μM. Anti-infective agent 5 effectively reduces parasite burden in vivo. Anti-infective agent 5 can be used for the research of infection.

P-536 is a ACE inhibitor that also inhibits herpes simplex virus HSV-1 thymidine kinase and Trypanosoma cruzi RNA polymerase. By inhibiting the renin-angiotensin system, downregulating the expression of AT1R and NOX4, and reducing oxidative stress (decreasing plasma hydrogen peroxide (H₂O₂) and 8-isoprostaglandin levels), P-536 effectively reduces systolic blood pressure and improves vascular reactivity. P-536 also inhibits the replication of DNA/RNA viruses such as HSV-1 by blocking nucleotide metabolism and nucleic acid synthesis, competitively inhibits RNA synthesis in Trypanosoma cruzi, and inhibits amastigote replication, thereby impeding its growth. P-536 is suitable for research on hypertension, insulin resistance, and Chagas disease.

5,7,8-Trimethoxycoumarin is an anti-parasite agent with IC₅₀s of 25.5 μM and 57.7 μM against Trypanosoma cruzi and L. amazonensis, respectively.

DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.

Nifurtimox-d₄ is deuterium labeled Nifurtimox. Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).

Kukoamine A-d₈ (dihydrochloride) is deuterium labeled Kukoamine A. Kukoamine A is a natural occurring spermine derivative, acts as a potent inhibitor of trypanothione reductase (Ki, 1.8 μM), with antihypertensive activity.

Antiparasitic agent-14 is a potent antiparasitic agent. Antiparasitic agent-14 shows cytotoxicity and antiparasitic activity. Antiparasitic agent-14 inhibits the growth of trypomastigote and amastigote.

Antitrypanosomal agent 11 is an antitrypanosomal agent that inhibits Trypanosoma cruzi with an IC₅₀ of 0.23 μM.

Anti-Trypanosoma cruzi agent-1 (Compd E5) posseses anti-T. gondii activity.

CPN4F is a chalcone derivative with antiparasitic activity. CPN4F is an inhibitor of the cysteine protease cruzain. CPN4F forms a key hydrogen bond with the Trp-184 residue in the active site of parasitic cruzain as an electrophile, and induces oxidative stress, cell membrane degradation, and necrosis, thereby inhibiting parasite proliferation. CPN4F is used in research related to Chagas disease.

Euphorbadienol (alpha-Euphorbol), a triterpenic compound, isolated from the latex of Euphorbia resinifera. The derivatives of Euphorbadienol can be used as elicitors of disease resistance, and has antileishmanial and antitrypanosomal activity.

Anti-Trypanosoma cruzi agent-4 (compound 5c) is an inhibitor of Trypanosoma cruzi. Anti-Trypanosoma cruzi agent-4 can be used for the research of infection.

Antiparasitic agent-15, a pyridine-thiazolidinone, has anti-Trypanosoma cruzi and leishmanicidal activities. Antiparasitic agent-15 has IC₅₀s of 0.9 μM and 0.64 μM against trypomastigote and amastigote forms of T. cruzi. Antiparasitic agent-15 has IC₅₀s of 42.2 μM and 9.58 μM against trypomastigote and amastigote forms of L. amazonensis. Antiparasitic agent-15 induces parasite cell death through necrosis induction. Antiparasitic agent-15 induces morphological changes such as shortening, retraction and curvature of the parasite body and leakage of internal content with T. cruzi trypomastigotes.