Interaction of Monobenzamidine-Linked Trypanocides with the Trypanosoma brucei P2 Aminopurine Transporter
Open Access
- 1 December 2005
- journal article
- research article
- Published by American Society for Microbiology in Antimicrobial Agents and Chemotherapy
- Vol. 49 (12) , 5169-5171
- https://doi.org/10.1128/aac.49.12.5169-5171.2005
Abstract
Single benzamidine group-carrying compounds were shown to interact with the Trypanosoma brucei P2 aminopurine transporter. Replacement of the amidine with a guanidine group decreased affinity. Trypanocidal activity was evident, but compounds were equally toxic against trypanosomes lacking the P2 transporter, which indicates additional uptake routes for monobenzamidine-derived compounds.Keywords
This publication has 20 references indexed in Scilit:
- Design, synthesis and evaluation of potential inhibitors of HIV gp120–CD4 interactionsBioorganic & Medicinal Chemistry Letters, 2004
- Trypanocidal Activity of Melamine-Based NitroheterocyclesAntimicrobial Agents and Chemotherapy, 2004
- The Trypanocide Diminazene Aceturate Is Accumulated Predominantly through the TbAT1 Purine Transporter: Additional Insights on Diamidine Resistance in African TrypanosomesAntimicrobial Agents and Chemotherapy, 2004
- The trypanosomiasesThe Lancet, 2003
- Activity of Megazol, a Trypanocidal Nitroimidazole, Is Associated with DNA DamageAntimicrobial Agents and Chemotherapy, 2003
- The Biochemical Basis of Arsenical–Diamidine Crossresistance in African TrypanosomesParasitology Today, 1999
- Uptake of Diamidine Drugs by the P2 Nucleoside Transporter in Melarsen-sensitive and -resistant Trypanosoma brucei bruceiJournal of Biological Chemistry, 1995
- A diamidine-resistant Trypanosoma equiperdum clone contains a P2 purine transporter with reduced substrate affinityMolecular and Biochemical Parasitology, 1995
- Arsenical-resistant trypanosomes lack an unusual adenosine transporterNature, 1993