Synthesis and biological evaluation of isofolic acid

Article abstract of DOI:10.1021/jm00248a017

The synthesis of isofolic acid has been accomplished by utilizing an unambiguous procedure. A new ring closure reaction has been developed for construction of the isofolate framework and substituted pteridines in general. Isofolic acid and isopteroic acid were tested for their ability to inhibit the growth of 2 folate requiring strains of bacteria. Unlike homofolic acid, which is active only in the reduced form, isofolic acid derives its merit as one of the first folate analogs possessing a normal 2 amino 4 hydroxypteridine moiety showing remarkable antimetabolic activity per se.