Synthesis and radioprotective study of new siladithioacetals and germadithioacetals

Abstract

A series of organosilicon and organogermanium compounds derived from cysteamine, methylcysteamine and 2-[1-(1-naphthyl)ethyl]-2-imidazoline have been prepared and their radiopharmacological properties (radioprotective activity and toxicity) have been determined in mice. A number of these new organometallic derivatives have been found to possess radioprotective activity.We have also noted a notable decrease of the toxicity and a fairly large increase in the radioprotective activity in comparison with the unsubstituted organic molecules.

Synthesis and Radioprotective Effects of New Phosphorothioates Derived From Naphthylmethylimidazoline and Naphthylethylimidazoline

“…SCHEME 4 Structures of phosphorus derivatives obtained (11)(12)(13)(14)(15)(16)(17)(18)(19)(20). In order to determine the LD 50 of irradiation, we had to draw the straight line of mortality as a function of the decimal logarithm of the dose ( Figure 1).…”

Germaselenazolidines and germadiselenoacetals: syntheses and radioprotective properties

“…1 H NMR spectra were recorded on a Bruker AC-80 spectrometer (80.13 MHz) and 13 C NMR spectra on a Bruker AC-200 spectrometer (50.32 MHz). Chemical shifts are reported in parts per million relative to internal Me 4 Si as reference.…”

“…Conversely, in the case of the linear structures, the presence of a methyl group in α position to the selenium atom causes a reduction in the acute toxicity, just as observed in the case of sulfur. 13 Moreover, for the linear structures 5-8, and conversely with the cyclic derivatives 1-4, the derivative with the n-hexyl group is less toxic and more active than the derivative with the i-amyl group. We thus note that the contribution brought by the i-amyl and n-hexyl vectors is reversed when we pass from a cyclic structure to a linear structure.…”

Synthesis and radioprotective action of silathiazolidines and germathiazolidines

“…To a solution of N-substituted cysteamine (14; 2.51 g, 7.33 mmol) in 50 ml of THF was added dropwise with Metallathiazolidines used in this study: M = Ge (1-6), Si (7)(8)(9)(10)(11)(12); R = R = n-C 6 H 13 ; R = H (1, 7); R = R = n-C 6 H 13 ; R = CH 3 (2, 8); R = R = i-C 5 H 11 ; R = H (3, 9); R = R = i-C 5 H 11 ; R = CH 3 (4, 10); R = CH 3 ; R = p-CH 3 C 6 H 4 ; R = H (5, 11); R = CH 3 ; R = p-CH 3 C 6 H 4 ; R = CH 3 (6,12). stirring a solution of bis(diethylamino)dihexylsilane (2.40 g, 7.33 mmol) in 50 ml of anhydrous THF.…”