Synthesis of novel benzamidine- and guanidine-derived polyazamacrocycles: Selective anti-protozoal activity for human African trypanosomiasis.

Abstract

Efficient synthetic routes have been developed for the preparation of two new polyazamacrocycles tagged with structural motifs recognised by the Trypanosoma brucei P2 aminopurine transporter. Biological testing of these compounds showed highly selective anti-protozoal activity against trypanosomes.

• Authors: Caroline M Reid, Charles Ebikeme, Michael P Barrett, Eva-Maria Patzewitz, Sylke Müller, David J Robins, Andrew Sutherland
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 18 Issue 20 Pg. 5399-401 (Oct 15 2008) ISSN: 1464-3405 [Electronic] England
• PMID: 18829314 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antiprotozoal Agents
• Benzamidines
• Purines
• Guanidine
• benzamidine

Topics

• Amino Acid Motifs
• Animals
• Antiprotozoal Agents (pharmacology)
• Benzamidines (chemistry)
• Biological Transport
• Cell Line
• Chemistry, Pharmaceutical (methods)
• Drug Design
• Guanidine (chemistry)
• Humans
• Models, Chemical
• Plasmodium falciparum (metabolism)
• Purines (chemistry)
• Trypanosomiasis, African (drug therapy, metabolism)