Synthesis and Biological Evaluation of 5-Arylfuro[2, 3-d]pyrimidines as Novel Dihydrofolate Reductase Inhibitors

Abstract

A series of about fifty novel 5-arylfuro[2, 3-d]pyrimidine derivatives were synthesized as potential inhibitors of dihydrofolate reductase (DHFR) arising from different species. Weak enzyme inhibition was observed for most of the compounds, with only a few reaching IC₅₀ values less than 30 μM. With regards to antibacterial and antimalarial potency, only seven compounds showed a modest in vitro activity against some bacterial strains and only three products proved significantly active against P. falciparum.