Glutamine analogues containing a keto function – novel inhibitors of fungal glucosamine-6-phosphate synthase

Abstract

A series of novel inhibitors of glucosamine-6-phosphate synthase, analogues of AADP and BADP, have been synthesized and their inhibitory, lipophilic and antifungal properties have been tested. The improvement in lipophilicity has not much affected the antifungal activity of the new compounds. Dipeptides containing norvaline and selected inhibitors have shown substantial activity against S. cerevisiae and C. glabrata and only poor activity against C. albicans strain. These peptides do not seem to be toxic towards human cells.

Keywords::

• Antifungal agents
• glucosamine-6-phosphate synthase inhibitors
• AADP analogues
• BADP analogues

Acknowledgements

This work was supported by the Ministry of Science and Information Society Technologies, Grant No. 2PO5F 014 26 and in part Grant No. 3PO5F02324.