Heterocyclic Thiosemicarbazones Research Articles

Heterocyclic Thiosemicarbazones: Correlation Between Structure, Inhibition of Ribonucleotide Reductase, and Inhibition of DNA Viruses

SummaryThe thiosemicarbazones of 2-formylpyridine, 3-formylpyridine, 4-for-mylpyridine, 5-hydroxy-2-formylpyridine, 1-formylisoquinoline, 5-hydroxy-1-formylisoquinoline, 6-formylpurine, isatin, and 1-methylisatin were examined for activity against herpes simplex virus in H.Ep.−2 cells and human cytomegalovirus in WI-38 cells, and also for inhibition of ribonucleotide reductase activity in H.Ep.−2 cells. A correlation was seen between inhibition of reductase and antiviral activity, with those compounds having the -CH=N-NH-C(=S) -NH2 moiety affixed to the heterocyclic ring system in the position alpha to the ring nitrogen being active. The suggestion is made that the activity of ribonucleotide reductase may be a limiting factor in the replication of certain members of the herpesvirus group.

A controlled clinical trial of isoniazid and heterocyclic thiosemicarbazone compared with isoniazid and pas in pulmonary tuberculosis

The study concerns the therapeutic results in 117 previously untreated patients with open pulmonary tuberculosis. The patients were randomly allocated to four groups treated with either 300 mg. isoniazid (INH) plus 12 g. of sodium PAS, or 300 mg. isoniazid plus 150. mg. of heterocyclic thiosemicarbazone (HTSC), or 450 mg. isoniazid plus 150 mg. HTSC. or 450 mg. isoniazid plus 100 mg. HTSC. The drugs were given in three equal doses daily.

Über einige heterozyklische Thiosemicarbazone

Description of 30 thiosemicarbazones of heterocyclic Aldehydes. Some of these compounds show tuberculostatic activityin vivo superior to p-Acetylaminobenzal-dehyde-thiosemicarbazone which statement was already made independently by French and American research groups. In the series of heterocyclic thiosemicarbazones very small changes in the molecular structure may cause a total loss of the tuberculostatic properties.