Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria
- Bioorg Med Chem Lett. 2003 Dec 1;13(23):4217-21. doi: 10.1016/j.bmcl.2003.07.023.
- 1. Arpida Ltd, Dammstrasse 36, CH-4142, Muenchenstein, Switzerland. [email protected]
Iclaprim, a new selective dihydrofolate inhibitor was synthesized based on rational drug design. Iclaprim's interaction with a resistant Staphylococcus aureus dihydrofolate reductase (DHFR) is outlined in comparison to trimethoprim (TMP). This compound is active against methicillin, TMP and vancomycin resistant strains. Arpida Ltd. is developing Iclaprim for serious hospital infections from Gram-positive pathogens and respiratory tract infections.