A fluorinated phenylbenzothiazole arrest the Trypanosoma cruzi cell cycle and diminishes the mammalian host-cell infection.

A fluorinated phenylbenzothiazole arrest the Trypanosoma cruzi cell cycle and diminishes the mammalian host-cell infection. Antimicrob Agents Chemother. 2019 Nov 11;: Authors: Cuevas-Hernández RI, Girard RMBM, Martínez-Cerón S, Santos da Silva M, Elias MC, Crispim M, Trujillo-Ferrara JG, Silber AM Abstract Chagas disease (CD) is a human infection caused by Trypanosoma cruzi CD was traditionally endemic to the Americas, however, due to migration it has spread to non-endemic countries. The current chemotherapy to treat CD induce several side effects and its effectiveness in the chronic phase of the disease is controversial. In this contribution, substituted phenylbenzothiazole derivatives were synthesized and biologically evaluated as trypanocidal agents against Trypanosoma cruzi The trypanocidal activities of the most promising compounds were determined through systematic in vitro screening and their mode of action as well. The physicochemical-structural characteristics responsible for the trypanocidal effects were identified, and their possible therapeutic application in Chagas disease is discussed. Our results show that the fluorinated compound, 2-methoxy-4-[5-(trifluoromethyl)-1,3-benzothiazol-2-yl] phenol (BT10) has the ability to inhibit the proliferation of epimastigotes (IC50(Epi) = 23.1 ± 1.75 μM) and intracellular forms trypomastigote (IC50(Tryp) = 8.5 ± 2.9 μM) and diminishes the infection index by more than 80%. In a...
Source: Antimicrobial Agents and Chemotherapy - Category: Microbiology Authors: Tags: Antimicrob Agents Chemother Source Type: research