Accession Number:

ADA023434

Title:

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

Descriptive Note:

Final rept. 1 Sep 72-31 Dec 74.

Corporate Author:

BOYCE THOMPSON INST FOR PLANT RESEARCH INC YONKERS N Y

Personal Author(s):

Report Date:

1975-09-30

Pagination or Media Count:

45.0

Abstract:

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

Subject Categories:

  • Pharmacology

Distribution Statement:

APPROVED FOR PUBLIC RELEASE