Radioprotective action of thiadiazole derivatives
Continuing previous investigations on the search for radioprotectors among the sulfurcontaining heterocycles [i, 2], we synthesized and studied the radioprotective properties of derivatives of 1,3,4and 1,2,4-thiadiazoles with various substituents: amino groups, alkyls, and mercapto groups. The following thiadiazole derivatives were investigated: 2alkylamino-5-alkyl-l,3,4-thiadiazoles and their methiodides (I-VII); 2-alkylamino-l,3,4thiadiazole-5-thiones (VIII-XII); 2-alkylamino-5-alkylmercapto-l,3,4-thiadiazoles (XIIIXVIII); 2,5-diamino-l,3,4-thiadiazole and its methiodide (XIX, XX), and 1,2,4-thiadiazoles (XXI-XXIII).
The radioprotective action of guanylthiourea and related compounds.
SummaryCompounds incorporating the thioureido and guanidino structures have been tested for protective action against 900 r whole-body x-radiation in mice. Guanylthiourea (toluene-p-sulphonate) gave 66 per cent survival at 30 days. The more toxic oxidation product, 3,5-diamino-1,2,4-thiadiazole was four times more effective on a molar basis and gave 69 per cent survival. Substituted derivatives and analogues were less protective. Autopsies and histological studies demonstrated little reduction of intestinal causes of death but considerable protection of the bone-marrow. It seems likely that these compounds have a similar mode of action to AET and cysteamine.
Darstellung und Eigenschaften des 1.2.4‐ und des 1.3.4‐Thiodiazols
Aus 5-Amino-1.2.4-thiodiazol und 2-Amino-1.3.4-thiodiazol sowie ihren C-Methyl-Derivaten wurden uber die entsprechenden Brom (Chlor)-thiodiazole die bisher unbekannten Grundkorper der beiden Thiodiazolreihen und ihre Methyl-Homologen dargestellt.