chagas

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.

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].

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.

GNF6702 is a selective inhibitor of the kinetoplastid proteasome and has been shown to be effective against parasites in mouse models of leishmaniasis, Chagas disease and human African trypanosomiasis.

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].

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

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

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].

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.

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.

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