Synthesis, in vitro antitrypanosomal and antibacterial activity of phenoxy, phenylthio or benzyloxy substituted quinolones

Chagas' disease, caused by Trypanosoma cruzi (T. cruzi), is one of the most serious parasitic diseases in Latin America. The currently available chemotherapy, based on nifurtimox or benznidazole, is unsatisfactory due to the limited efficacy in the prevalent chronic stage of the disease and toxic side effects. In order to address these deficiencies, a series of quinolones based novel molecules have been synthesized and evaluated as potential antitrypanosomal agents. The most active analogue 10 inhibited T. cruzi with an IC50 of 1.3 mu g/mL. The results of this study have implications in the development of novel quinolone's antitrypanosomal agents. (C) 2008 Elsevier Ltd. All rights reserved.