Efficacy of Novel Pyrazolone Phosphodiesterase Inhibitors in Experimental Mouse Models of Trypanosoma cruzi

Autor: de Araújo, Julianna Siciliano, França da Silva, Cristiane, Batista, Denise da Gama Jaén, Nefertiti, Aline, Fiuza, Ludmila Ferreira de Almeida, Fonseca-Berzal, Cristina Rosa, Bernardino da Silva, Patrícia, Batista, Marcos Meuser, Sijm, Maarten, Kalejaiye, Titilola D., de Koning, Harry P., Maes, Louis, Sterk, Geert Jan, Leurs, Rob, Soeiro, Maria de Nazaré Correia
Zdroj: Antimicrobial Agents and Chemotherapy; July 2020, Vol. 64 Issue: 9
Abstrakt: Pyrazolones are heterocyclic compounds with interesting biological properties. Some derivatives inhibit phosphodiesterases (PDEs) and thereby increase the cellular concentration of cyclic AMP (cAMP), which plays a vital role in the control of metabolism in eukaryotic cells, including the protozoan Trypanosoma cruzi, the etiological agent of Chagas disease (CD), a major neglected tropical disease. In vitrophenotypic screening identified a 4-bromophenyl-dihydropyrazole dimer as an anti-T. cruzihit and 17 novel pyrazolone analogues with variations on the phenyl ring were investigated in a panel of phenotypic laboratory models.
Databáze: Supplemental Index