Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives

  • Bioorg Med Chem Lett. 2011 Oct 1;21(19):5804-7. doi: 10.1016/j.bmcl.2011.07.112.
Xue-Liang Shi  1 ,  Jian-Feng Ge ,  Bao-Qiang Liu ,  Marcel Kaiser ,  Sergio Wittlin ,  Reto Brun ,  Masataka Ihara
Affiliations
  • 1. Key Laboratory of Organic Synthesis of Jiangsu Province, Soochow University, 199 Ren'Ai Road, Suzhou 215123, China.
PMID: 21868222 DOI: 10.1016/j.bmcl.2011.07.112
Abstract

A series of 5-phenyliminobenzo[a]phenoxazine derivatives were synthesized. The in vitro antiprotozoal activities were evaluated against Plasmodium falciparum K1, Trypanosoma cruzi, Leishmania donovani and Trypanosoma brucei rhodesiense. N,N-Diethyl-5-((4-methoxyphenyl)imino)-5H-benzo[a]phenoxazin-9-amine shows IC(50)=0.040 μmol L(-1) with a selective index of 1425 against Plasmodium falciparum K1.