title: New antiprotozoal agents: their synthesis and biological evaluations.
abstract: 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 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.
authors.affiliation: Program of Chemical Biology, Institute of Cell and Molecular Biology, Biomedical Centre, Uppsala University, SE-75123 Uppsala, Sweden. ram@boc.uu.se
authors.forename: Ram Shankar
authors.initials: RS
authors.lastname: Upadhayaya
authors.forename: Shailesh S
authors.initials: SS
authors.lastname: Dixit
authors.forename: Andras
authors.initials: A
authors.lastname: Földesi
authors.forename: Jyoti
authors.initials: J
authors.lastname: Chattopadhyaya
mesh_terms: D000666:Amphotericin B / Q000737:chemistry / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D018314:Leishmania infantum / Q000187:drug effects; D009547:Nifurtimox / Q000737:chemistry / Q000494:pharmacology; D009593:Nitroimidazoles / Q000737:chemistry / Q000494:pharmacology; D021261:Parasitic Sensitivity Tests; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000981:Antiprotozoal Agents; D009593:Nitroimidazoles; D011804:Quinolines; D000666:Amphotericin B; D009547:Nifurtimox; C009999:benzonidazole