Development of a novel class of pyrrolo-[1,2,5]benzothiadiazepine derivatives as potential anti-schistosomal agents

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3785-7. doi: 10.1016/j.bmcl.2013.04.085. Epub 2013 May 9.

Abstract

Analogues of pyrrolo-[1,2,5]benzothiadiazepine were prepared and evaluated against Schistosoma japonica. The biological data revealed that most benzothiazepine derivatives show anti-schistosomal activity to some extent, while α-chloronation of the title compound and another bioisosteric derivative pyrrolo-[1,2,5]benzodiazepine displayed the most distinct worm killing activity. This study proved that benzodiazepine may serve as a novel structural skeleton for the development of anti-schistosomal agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drug Design*
  • Molecular Structure
  • Pyrroles / chemical synthesis
  • Pyrroles / chemistry
  • Pyrroles / pharmacology*
  • Schistosoma japonicum / drug effects*
  • Structure-Activity Relationship
  • Thiazepines / chemical synthesis
  • Thiazepines / chemistry
  • Thiazepines / pharmacology*

Substances

  • Pyrroles
  • Thiazepines