Synthesis and biological evaluation of quinones derived from natural product komaroviquinone as anti-Trypanosoma cruzi agents

  • Bioorg Med Chem Lett. 2015 Aug 1;25(15):2967-71. doi: 10.1016/j.bmcl.2015.05.022.
Yutaka Suto  1 ,  Junko Nakajima-Shimada  2 ,  Noriyuki Yamagiwa  3 ,  Yoko Onizuka  2 ,  Genji Iwasaki  3
Affiliations
  • 1. Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan. Electronic address: [email protected].
  • 2. Department of Molecular and Cellular Parasitology, Graduate School of Health Sciences, Gunma University, Maebashi 371-8514, Japan.
  • 3. Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki 370-0033, Japan.
PMID: 26037321 DOI: 10.1016/j.bmcl.2015.05.022
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.

Keywords
Chagas’ disease; Quinone; Trypanosoma cruzi.