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Infectious disease


Dihydrofolate reductase (DHFR); pteridine reductase (PTR1)

Cell culture studies identified piperidine-pteridine-based PTR1 inhibitors that could help circumvent antifolate drug resistance associated with Leishmania infection. Leishmania can overcome DHFR inhibition by overexpressing PTR1. In two strains of Leishmania, members of the PTR1 inhibitor series increased pyrimethamine-mediated growth inhibition compared with pyrimethamine alone. Next steps include testing optimized versions of the identified PTR1 inhibitors in combination with DHFR inhibitors in mouse models.
Pyrimethamine is a generic DHFR inhibitor used to treat protozoan infections.

SciBX 5(38); doi:10.1038/scibx.2012.1007
Published online Sept. 27, 2012

Patent pending; available for licensing from Tydock Pharma srl

Cornona, P. et al. J. Med. Chem.; published online Aug. 14, 2012;
Contact: Maria Paola Costi, University of Modena and Reggio Emilia, Modena, Italy