New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms.
New oxirane derivatives were synthesized using six naphthoquinones as the starting materials. Our biological results showed that these oxiranes acted as trypanocidal agents against Trypanosoma cruzi with minimal cytotoxicity in the VERO cell line compared to naphthoquinones. In particular, oxirane derivative 14 showed low cytotoxicity in a mammalian cell line and exhibited better activity against epimastigote forms of T.cruzi than the current drug used to treat Chagas disease, benznidazole.
Universidade Federal do Rio de Janeiro, Núcleo de Pesquisas de Produtos Naturais, 21944-970 Cidade Universitária, RJ, Brazil.
Paula F
PF
Carneiro
Samara B
SB
do Nascimento
Antonio V
AV
Pinto
Maria do Carmo F R
Mdo C
Pinto
Guilherme C
GC
Lechuga
Dilvani O
DO
Santos
Helvécio M
HM
dos Santos Júnior
Jackson A L C
JA
Resende
Saulo C
SC
Bourguignon
Vitor F
VF
Ferreira
D000818:Animals; D016923:Cell Death / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005027:Ethylene Oxide / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D009285:Naphthoquinones / Q000737:chemistry* / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000166:cytology / Q000187:drug effects* / Q000254:growth & development; D014709:Vero Cells
D009285:Naphthoquinones; D014344:Trypanocidal Agents; D005027:Ethylene Oxide; C035342:1,4-naphthoquinone