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New antiprotozoal agents: Their synthesis and biological evaluations
Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Cell and Molecular Biology, Chemical Biology.
Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Cell and Molecular Biology, Chemical Biology.
Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Cell and Molecular Biology, Chemical Biology.
Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Cell and Molecular Biology, Chemical Biology.
2013 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1090-2120, Vol. 23, no 9, 2750-2758 p.Article in journal (Refereed) Published
Abstract [en]

Here 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 mu M. 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. 

Place, publisher, year, edition, pages
2013. Vol. 23, no 9, 2750-2758 p.
Keyword [en]
Antiprotozoal agents, Trypanosoma, Leishmania, Parasite inhibitors, Conformationally constrained quinoline
National Category
Natural Sciences
Identifiers
URN: urn:nbn:se:uu:diva-200043DOI: 10.1016/j.bmcl.2013.02.054ISI: 000317333900054OAI: oai:DiVA.org:uu-200043DiVA: diva2:622938
Available from: 2013-05-23 Created: 2013-05-20 Last updated: 2017-12-06Bibliographically approved

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Upadhayaya, Ram ShankarDixit, Shailesh S.Földesi, AndrásChattopadhyaya, Jyoti

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