Synthesis of ethyl 5-phenyl-6-oxa-1-azabicyclo[3.1.0]hexane-2-carboxylate derivatives and evaluation of their antimalarial activities

  • J Med Chem. 2003 Jun 5;46(12):2397-403. doi: 10.1021/jm020452h.
Nongpanga Ningsanont  1 ,  David St C Black ,  Rachada Chanphen ,  Yodhathai Thebtaranonth
Affiliations
  • 1. Department of Chemistry, Faculty of Science, Mahidol University, Rama 6 Road, Bangkok 10400, Thailand.
PMID: 12773043 DOI: 10.1021/jm020452h
Abstract

Derivatives of ethyl 5-phenyl-6-oxa-1-azabicyclo[3.1.0]hexane-2-carboxylate (14-20), with side chains varying from three to five carbon atoms and bearing various substituents, have been prepared from ethyl 2-phenyl-1-pyrroline-5-carboxylate (12). Their in vitro activity against P. falciparum (K1 strain) and antimycobacterium and also their cytotoxic activity against Vero cell have been evaluated.