Synthesis and antimalarial activity of novel chiral and achiral benzenesulfonamides bearing 1, 3, 4-oxadiazole moieties

Abstract

A series of new benzenesulfonamides, most of which are chiral, incorporating 1, 3, 4-oxadiazole and amino acid moieties have been synthesized. Some of these compounds were screened for antimalarial activity and also evaluated for their ability to inhibit hem polymerization. The electrophoretic analysis indicated that one compound was effective in inhibiting the degradation of hemoglobin. The synthesized compounds were tested in mice infected with Plasmodium berghei. These derivatives have the potential for the development of novel antimalarial lead compounds.

Keywords::

• Chiral benzenesulfonamides
• 1,3,4-oxadiazole
• antimalarial activity
• parasitaemia
• electrophoretic analysis

Acknowledgements

The authors wish to express their sincere thanks to Prof. Jose N. Dominguez, Laboratorio de Bioquimica. Facultad de Farmacia. Universidad Central de Venezuela, for conducting the antimalarial studies.