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. 2003 Dec 1;13(23):4217-21.
doi: 10.1016/j.bmcl.2003.07.023.

Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria

Peter Schneider  1 , Stephen Hawser, Khalid Islam
Affiliations

Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria

Peter Schneider et al. Bioorg Med Chem Lett. .

Abstract

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.

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