2-Acetylpyridine thiosemicarbazones. 4. Complexes with transition metals as antimalarial and antileukemic agents

Reaction of the 2-acetylpyridine thiosemicarbazones, 3-azabicyclo[3.2.2]nonane-3-thiocarboxylic acid 2-[1-(2-pyridyl)ethylidene]hydrazide (IIIa), its selenium analogue (IIIb), 1H-hexahydroazepine-1-thiocarboxylic acid 2-[1-(2-pyridyl)ethylidene]hydrazide (IV), and 1H-octahydroazocine-1-thiocarboxyli...

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Veröffentlicht in:Journal of medicinal chemistry 1982-10, Vol.25 (10), p.1261-1264
Hauptverfasser: Scovill, John P, Klayman, Daniel L, Franchino, Charles F
Format: Artikel
Sprache:eng
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Zusammenfassung:Reaction of the 2-acetylpyridine thiosemicarbazones, 3-azabicyclo[3.2.2]nonane-3-thiocarboxylic acid 2-[1-(2-pyridyl)ethylidene]hydrazide (IIIa), its selenium analogue (IIIb), 1H-hexahydroazepine-1-thiocarboxylic acid 2-[1-(2-pyridyl)ethylidene]hydrazide (IV), and 1H-octahydroazocine-1-thiocarboxylic acid 2-[1-(2-pyridyl)ethylidene]hydrazide (V) with Cu(II), Ni(II), Fe(III), and Mn(II) salts gave crystalline complexes. Relative to the free ligands, these complexes show reduced antimalarial activity in mice infected with Plasmodium berghei; however, antileukemic properties are enhanced by coordination with the above-mentioned metals.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00352a036