Beltran-Hortelano, Ivan’s team published research in European Journal of Medicinal Chemistry in 2021-11-05 | CAS: 1468-83-3

European Journal of Medicinal Chemistry published new progress about Chagas disease. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Quality Control of 1468-83-3.

Beltran-Hortelano, Ivan published the artcileDesign and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease, Quality Control of 1468-83-3, the main research area is synthesis Mannich base imidazole benzimidazole drug discovery Chagas disease; drug design treatment Chagas disease Mannich base; Benzimidazole; Chagas disease; Imidazole; Mannich bases; Neglected tropical diseases; Trypanosoma cruzi.

The protozoan parasite Trypanosoma cruzi is the causative agent of Chagas disease, the most important parasitic infection in Latin America. The only treatments currently available are nitro-derivative drugs that are characterized by high toxicity and limited efficacy. Therefore, there is an urgent need for more effective, less toxic therapeutic agents. We have previously identified the potential for Mannich base derivatives as novel inhibitors of this parasite. To further explore this family of compounds, we synthesized a panel of 69 new analogs, based on multi-parametric structure-activity relationships, which allowed optimization of both anti-parasitic activity, physicochem. parameters and ADME properties. Addnl., we optimized our in vitro screening approaches against all three developmental forms of the parasite, allowing us to discard the least effective and trypanostatic derivatives at an early stage. We ultimately identified derivative I, which demonstrated excellent trypanocidal properties, and a synergistic mode of action against trypomastigotes in combination with the reference drug benznidazole. Both its druggability and low-cost production make this derivative a promising candidate for the preclin., in vivo assays of the Chagas disease drug-discovery pipeline.

European Journal of Medicinal Chemistry published new progress about Chagas disease. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Quality Control of 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem