Ram Shankar Upadhayaya, Shailesh S Dixit, Andras Földesi, Jyoti Chattopadhyaya
Program of Chemical Biology, Institute of Cell and Molecular Biology, Biomedical Centre, Uppsala University, SE-75123 Uppsala, Sweden. ram@boc.uu.se
Bioorganic & medicinal chemistry letters 2013 May 1Here we report identification of new lead compounds based on quinoline and indenoquinolines with variable side chains as antiprotozoal agents. Quinolines 32, 36 and 37 (Table 1) and indenoquinoline derivatives 14 and 23 (Table 2) inhibit the in vitro growth of the Trypanosoma cruzi, Trypanosoma brucei, Trypanosoma brucei rhodesiense subspecies and Leishmania infantum with IC50=0.25 μM. These five compounds have superior activity to that of the front-line drugs such as benznidazole, nifurtimox and comparable to amphotericin B. Thus these compounds constitute new 'leads' for further structure-activity studies as potential active antiprotozoal agents. Copyright © 2013 Elsevier Ltd. All rights reserved.
Ram Shankar Upadhayaya, Shailesh S Dixit, Andras Földesi, Jyoti Chattopadhyaya. New antiprotozoal agents: their synthesis and biological evaluations. Bioorganic & medicinal chemistry letters. 2013 May 1;23(9):2750-8
PMID: 23518280
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