Synthesis,in vitro antitrypanosomal and antibacterial activity of phenoxy,phenylthio or benzyloxy substituted quinolones |
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| Authors: | Xiang Ma Weicheng Zhou Reto Brun |
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| Affiliation: | 1. State Key Lab of New Drug & Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, 1111 North Zhongshan Road, Shanghai 200437, PR China;2. Department of Chemical and Biomolecular Engineering, National University of Singapore, 4 Engineering Drive 4, B1k E5 #02-09, Singapore 117576, Singapore;3. Medical Parasitology and Infection Biology, Parasite Chemotherapy, Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland |
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| Abstract: | 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 μg/mL. The results of this study have implications in the development of novel quinolone’s antitrypanosomal agents. |
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