Reverse-benzamidine antimalarial agents: design, synthesis, and biological evaluation

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5815-7. doi: 10.1016/j.bmcl.2010.07.124. Epub 2010 Aug 3.

Abstract

In the frame of the development of bis-cationic choline analogs, the RSA of bis-N-alkylamidines were studied and a new series of reverse-benzamidine derivatives was designed. Contrary to the lipophilicity, the basicity of alkylamidine compounds directly influences their antimalarial potencies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology
  • Benzamidines / chemical synthesis*
  • Benzamidines / chemistry
  • Benzamidines / pharmacology
  • Drug Design
  • Plasmodium falciparum / drug effects
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Benzamidines