Synthesis of Site-Directed Chelating Agents I: Pteridine Carboxaldehyde Thiosemicarbazones

Several 6-formylpteridine thiosemicarbazones and semi-carbazones were synthesized as potential inhibitors of the enzyme dihydrofolate reductase. The most active derivative in this series was 2,4-diaminopteridine-6-carboxaldehyde semicarbazone, which caused 50% inhibition of dihydrofolate reductase o...

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Veröffentlicht in:	Journal of pharmaceutical sciences 1973-01, Vol.62 (1), p.150-151
Hauptverfasser:	Hochman, Howard I., Agrawal, Krishna C., Shansky, Charles W., Sartorelli, Alan C.
Format:	Artikel
Sprache:	eng
Schlagworte:	6-Formylpteridine thiosemicarbazones and semicarbazones-synthesized and tested as site-directed chelating agents of dihydrofolate reductase Aldehydes - chemical synthesis Binding Sites Chelating Agents - chemical synthesis Dihydrofolate reductase-synthesis and testing of pteridine carboxaldehyde thiosemicarbazones as potential inhibitors Folic Acid Antagonists Humans In Vitro Techniques Liver - drug effects Liver - enzymology Pteridine carboxaldehyde thiosemicarbazones-synthesized and tested as site-directed chelating agents of dihydrofolate reductase Pteridines - chemical synthesis Tetrahydrofolate Dehydrogenase - isolation & purification Thiosemicarbazones - chemical synthesis
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Beschreibung
Zusammenfassung:	Several 6-formylpteridine thiosemicarbazones and semi-carbazones were synthesized as potential inhibitors of the enzyme dihydrofolate reductase. The most active derivative in this series was 2,4-diaminopteridine-6-carboxaldehyde semicarbazone, which caused 50% inhibition of dihydrofolate reductase of human liver at a concentration of 1.4 × 10−7M.
ISSN:	0022-3549 1520-6017
DOI:	10.1002/jps.2600620135