New antiprotozoal agents: Their synthesis and biological evaluations
2013 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1464-3405, Vol. 23, no 9, 2750-2758 p.Article in journal (Refereed) Published
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.
Antiprotozoal agents, Trypanosoma, Leishmania, Parasite inhibitors, Conformationally constrained quinoline
IdentifiersURN: urn:nbn:se:uu:diva-200043DOI: 10.1016/j.bmcl.2013.02.054ISI: 000317333900054OAI: oai:DiVA.org:uu-200043DiVA: diva2:622938