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

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Schneider P, Hawser S, Islam K

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

Bioorg Med Chem Lett. 2003 Dec 1;13(23):4217-21.

PubMed ID
14623005 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drugs
Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
TrimethoprimDihydrofolate reductaseIC 50 (nM)>300000730Details