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New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2012 Aug 15; Vol. 20 (16), pp. 4995-5000. Date of Electronic Publication: 2012 Jun 21. - Publication Year :
- 2012
-
Abstract
- 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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Cell Death drug effects
Cell Survival drug effects
Chlorocebus aethiops
Dose-Response Relationship, Drug
Drug Evaluation, Preclinical
Ethylene Oxide analogs & derivatives
Ethylene Oxide chemistry
Models, Molecular
Molecular Structure
Parasitic Sensitivity Tests
Structure-Activity Relationship
Trypanocidal Agents chemical synthesis
Trypanosoma cruzi cytology
Trypanosoma cruzi growth & development
Vero Cells
Ethylene Oxide pharmacology
Naphthoquinones chemistry
Naphthoquinones pharmacology
Trypanocidal Agents chemistry
Trypanocidal Agents pharmacology
Trypanosoma cruzi drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 20
- Issue :
- 16
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22795899
- Full Text :
- https://doi.org/10.1016/j.bmc.2012.06.027