chagas

T.cruzi-IN-1 (MDK1088) is a Trypanosoma cruzi inhibitor.

Albaconazole (W-0027) is a small molecule fungal cytochrome P450 family member 51 (fungal CYP51A1) inhibitor. It is used in the treatment of fungal infections, skin and musculoskeletal disorders, and can be used in the study of vulvovaginal candidiasis, Chagas disease and genitourinary disorders.

Se2h is a cruzain inhibitor exhibiting potent activity against intracellular amastigotes of Trypanosoma cruzi (EC50< 1 μM, SI> 10), with an inhibitory effect on cruzain of IC50< 100 nM (SI> 5.55). Compared to Benznidazole and cruzain inhibitor K777, Se2h shows superior selectivity and inhibition while its selenazole structure reduces selenium-related toxicity. Se2h demonstrates antiparasitic activity and holds promise for Chagas disease research.

CZP-IN-1 (compound SH-1) is an inhibitor targeting the pathogen Trypanosoma cruzi protease (CZP) without affecting cathepsin L (IC50=28 nM). This compound is applicable in Chagas disease research.

BiPNQ is a Trypanosoma cruzi inhibitor. Trypanosoma cruzi is the etiological agent of Chagas disease (American trypanosomiasis).

Megazol is a nitroimidazole based drug that cures some protozoan infections. A study of nitroimidazoles found the drug extremely effective against T. cruzi and T. brucei which cause Chagas disease and African sleeping sickness, respectively.

DB-766 is a potential chemotherapeutic candidate for Chagas' disease treatment. DB-766 exhibits strong trypanocidal activity and excellent selectivity for bloodstream trypomastigotes and intracellular amastigotes (Y strain), giving IC(50)s of 60 and 25 nM

GNF6702 is a selective inhibitor of the kinetoplastid proteasome, demonstrating efficacy against parasites in mouse models of leishmaniasis, Chagas disease, and human African trypanosomiasis.

WRR-483, an analogue of K-11777, is a potent and selective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777. WRR-483 demonstrates good potency against cruzain with sensitivity to pH conditions and high efficacy in the cell culture assay. Furthermore, WRR-483 also eradicates parasite infection in a mouse model of acute Chagas' disease. WRR-483 binds covalently to the active site cysteine of the protease in a similar manner as other vinyl sulfone-based inhibitors. WRR-483 has potential to be developed as a treatment for Chagas' disease.

Mammea A BA demonstrates significant efficacy in inhibiting Trypanosoma cruzi (T. cruzi), through mechanisms such as mitochondrial dysfunction, increased production of reactive oxygen species (ROS), and DNA fragmentation, alongside elevating acidic vacuole numbers. This compound is capable of inducing apoptosis, autophagy, and necrosis, making it a valuable research tool for Chagas disease.

AN15368, an orally administered small-molecule precursor, undergoes activation by parasite carboxypeptidase, yielding a product that interferes with the messenger RNA processing pathway in T. cruzi. This compound shows promise for both preventing and investigating potential treatments for Chagas disease [1].

Antitrypanosomal Agent 15 (Compound 26) is an orally active, brain-penetrant, selective inhibitor of the Trypanosoma cruzi proteasome, exhibiting a pIC50 of 7.4 for T. cruzi and <4 for the human proteasome. It possesses favorable ADME properties, rendering it useful for the study of Chagas disease [1].

Topoisomerase II Inhibitor 16 (compound CT3) is a selective, orally bioavailable, and irreversible inhibitor of trypanosomal topoisomerase II, possessing the ability to penetrate the brain and stabilize double-stranded DNA-enzyme cleavage complexes. It shows promise for research into Chagas disease [1].