Article
Trypanocidal activity of melamine-based nitroheterocycles.
Antimicrobial agents and chemotherapy - 1 May 2004
Stewart Mhairi L, Bueno Gorka Jimenez, Baliani Alessandro, Klenke Burkhard, Brun Reto, Brock Janice M, Gilbert Ian H, Barrett Michael P
Abstract excerpt
A series of nitroheterocyclic compounds were designed with linkages to melamine or benzamidine groups that are known substrates of the P2 aminopurine and other transporters in African trypanosomes of the brucei group. Several compounds showed in vitro trypanotoxicity with 50% inhibitory concentrations in the submicromolar range. Although most compounds interacted with the P2 transporter, as judged by their...
Topics
- Acetylglucosamine
- Animals
- Cell Line
- Drug Delivery Systems
- Female
- Heterocyclic Compounds
- Humans
- Mice
- Molecular Conformation
- Mutagens
- Mutation