Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives

  • J Med Chem. 2008 Jun 26;51(12):3654-8. doi: 10.1021/jm8003619.
Jian-Feng Ge  1 ,  Chika Arai ,  Marcel Kaiser ,  Sergio Wittlin ,  Reto Brun ,  Masataka Ihara
Affiliations
  • 1. Institute of Medicinal Chemistry, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan.
PMID: 18476684 DOI: 10.1021/jm8003619
Abstract

3,7-Bis(dialkylamino)phenoxazinium salts were synthesized and evaluated for in vitro activities against Plasmodium falciparum, Trypanosoma cruzi, T. brucei rhodesiense, and Leishmania donovani. Notably, the compounds showed potent antiprotozoal activities, especially against P. falciparum and T. cruzi. The compounds with alkyl side chains less than three carbons in length possessed good activities with high selective indices.