title: Synthesis and anti-Trypanosoma cruzi activity of β-lapachone analogues.
abstract: The available chemotherapy for Chagas disease, caused by Trypanosoma cruzi, is unsatisfactory; therefore, there is an intense effort to find new drugs for the treatment of this disease. In our laboratory, we have analyzed the effect on bloodstream trypomastigotes of 16 new naphthoquinone analogues of β-lapachone modified in the pyran ring, aiming to find a new prototype with high trypanocidal activity. The new compounds presented a broad spectrum of activity, and five of them presented IC(50)/24 h in the range of 22-63 μM, whereas β-lapachone had a higher value of 391.5 ± 16.5 μM.
authors: Departamento de Química Orgânica, Instituto de Química, UFRJ, 21949-900 Rio de Janeiro, RJ, Brazil.
authors: Sabrina Baptista
authors: SB
authors: Ferreira
authors: Kelly
authors: K
authors: Salomão
authors: Fernando
authors: F
authors: de Carvalho da Silva
authors: Antônio Ventura
authors: AV
authors: Pinto
authors: Carlos Roland
authors: CR
authors: Kaiser
authors: Angelo C
authors: AC
authors: Pinto
authors: Vitor Francisco
authors: VF
authors: Ferreira
authors: Solange L
authors: SL
authors: de Castro
mesh_terms: D000818:Animals; D001773:Blood Cells / Q000187:drug effects / Q000469:parasitology; D014355:Chagas Disease / Q000469:parasitology; D020128:Inhibitory Concentration 50; D008018:Life Cycle Stages / Q000187:drug effects* / Q000502:physiology; D051379:Mice; D009285:Naphthoquinones / Q000138:chemical synthesis* / Q000494:pharmacology; D011714:Pyrans / Q000737:chemistry; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development
chemical_list: D009285:Naphthoquinones; D011714:Pyrans; D014344:Trypanocidal Agents; C014638:beta-lapachone