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

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)

Document Details

Document Type
Technical Report
Publication Date
Sep 30, 1975
Accession Number
ADA023434

Entities

People

  • Herman Gershon

Organizations

  • Boyce Thompson Institute for Plant Research

Tags

DTIC Thesaurus Topics

  • Acidic Amino Acids
  • Amino Acids
  • Amino Acids Peptides And Proteins
  • Antimalarials
  • Aspartic Acid
  • Biological Pigments
  • Biomolecules
  • Chemical Compounds
  • Dicarboxylic Amino Acids
  • Glutamic Acid
  • Survival
  • Threonine

Fields of Study

  • Chemistry

Readers

  • Molecular and Cellular Biochemistry
  • Parasitology and Pharmacology of Malaria.