Methotrexate analogs. 6. Replacement of glutamic acid by various amino acid esters and amines
| Autor: | Edward J. Modest, Barbara L. Brown, Michael Chaykovsky |
|---|---|
| Rok vydání: | 1975 |
| Předmět: |
musculoskeletal diseases
chemistry.chemical_classification Chemistry Streptococcus Mice Inbred Strains Glutamic acid medicine.disease_cause Amino acid Mice Structure-Activity Relationship Methotrexate Glutamates Biochemistry In vivo Reagent Drug Discovery Enterococcus faecalis medicine Animals Molecular Medicine Moiety Leukemia L1210 Antibacterial activity medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 18:909-912 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00243a010 |
| Popis: | A series of methotrexate (MTX) analogs was prepared in which the glutamic acid moiety is replaced by various amino acid esters and amines. The synthetic method consisted of the reaction of 4-amino-4-deoxy-N10-methylpteroic acid with various reagents to form intermediate mixed anhydrides, which then reacted with amino acid esters or amines to give the MTX analogs. These compounds were tested for antibacterial activity against Streptococcus faecium and for antitumor activity against L1210 leukemia in mice. Several compounds showed significant antibacterial activity; the MTX homocysteinethiolactone and MTX aspartate analogs showed marginal in vivo antitumor activity. |
| Databáze: | OpenAIRE |
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