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Synthesis and biological evaluation of quinones derived from natural product komaroviquinone as anti-Trypanosoma cruzi agents.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Aug 01; Vol. 25 (15), pp. 2967-71. Date of Electronic Publication: 2015 May 16. - Publication Year :
- 2015
-
Abstract
- Current chemotherapy drugs for Chagas' disease are insufficient due to their limited efficacy; however, anti-trypanosomal agents have recently shown promise. As such, synthetic intermediates of komaroviquinone were evaluated for anti-trypanosomal activity. Based on the results, a series of novel quinone derivatives were screened for anti-trypanosomal activity and mammalian cytotoxicity. Several quinone derivatives displayed higher antiprotozoal activity against Trypanosoma cruzi trypomastigotes than the reference drug benznidazole, without concomitant toxicity toward the host cell.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- 3T3 Cells
Animals
Chagas Disease parasitology
Diterpenes chemical synthesis
Humans
Mice
Quinones chemical synthesis
Trypanocidal Agents chemical synthesis
Chagas Disease drug therapy
Diterpenes chemistry
Diterpenes pharmacology
Quinones chemistry
Quinones pharmacology
Trypanocidal Agents chemistry
Trypanocidal Agents pharmacology
Trypanosoma cruzi drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 25
- Issue :
- 15
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26037321
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.05.022