J Jonathan Nué-Martinez, David Cisneros, María Del Valle Moreno-Blázquez, Cristina Fonseca-Berzal, José Ignacio Manzano, Damien Kraeutler, Marzuq A Ungogo, Maha A Aloraini, Hamza A A Elati, Alexandra Ibáñez-Escribano, Laura Lagartera, Tomás Herraiz, Francisco Gamarro, Harry P de Koning, Alicia Gómez-Barrio, Christophe Dardonville
The AT-rich mitochondrial DNA (kDNA) of trypanosomatid parasites is a target of DNA minor groove binders. We report the synthesis, antiprotozoal screening, and SAR studies of three series of analogues of the known antiprotozoal kDNA binder 2-((4-(4-((4,5-dihydro-1 H -imidazol-3-ium-2-yl)amino)benzamido)phenyl)amino)-4,5-dihydro-1 H -imidazol-3-ium ( 1a ). Bis(2-aminoimidazolines) (1) and bis(2-aminobenzimidazoles) (2) showed micromolar range activity against Trypanosoma brucei, whereas bisarylimidamides (3) were submicromolar inhibitors of T...
September 20, 2023: Journal of Medicinal Chemistry