Folic Acid Analogs Containing Altered Glutamic Acid Residues as Potential Antimalarials. Dipeptides of O-Methyl-L-Threonine as Potential Antimalarials.

摘要

The following eight target compounds were prepared: Pteroyl aspartic acid, pteroyl 3-methylaspartic acid, pteroyl 3-methylglutamic acid, pteroyl 4-methylglutamic acid, pteroyl 3-phenylglutamic acid, pteroyl 4-phenylglutamic acid, pteroyl 2-amino-5-oxohexanoic acid, and pteroyl 2-amino-4-benzoylbutyric acid, along with 19 intermediates. In addition to this, four target dipeptides, L-Leucyl-L-leucine, L-leucyl-L-0-Methyl-threonine, L-0-methylthreonyl-L-leucine, and L-O-methylthreonyl-L-)-methylthreonine, along with 12 intermediates were synthesized. All of the compounds were screened against Plasmodium berghei in mice, and only L-O-methylthreonyl-L-O-methylthreonine prolonged survival time significantly. (Author)