SOME PROPERTIES OF 3,5-DISUBSTITUTED 1,2,4-TRIAZOLIUM HEXAFLUOROSILICATES

Abstract

Introduction

         Today as potential caries-preventive agents hexafluorosilicate ammonium and hexafluorosilicates organic "onium" cations actively studied, which have certain advantages over traditional means of fluoride treatment and prevention of tooth decay. Among these compounds are exposed to saliva hydrolysis to form a soluble form of silica that catalyzes the formation of phosphate sludge (fluoride) calcium and provides prolonged occlusion tubul dentin. As one of the most important physical and chemical characteristics of drugs is their solubility in water and hydrolytic instability, because the purpose of the present study investigated the solubility in water, hydrolytic instability and potential biological activity of 3,5-disubstituted 1,2,4-triazolium hexafluorosilicates in order to estimate their potential use as caries-preventive agents.

Investigation methods

         The method of synthesis hexafluorosilicates (LH)₂SiF₆ * nH₂O (L1 = 3-pyridine-3-yl-5- (2'-aminophenyl) -1H-1,2,4-triazole, n = 1; L2 = 3-benzofuran- 2-yl-5- (2'-amino-3'-methyl-phenyl) -1H-1,2,4-triazole, n = 1; L3 = 5- (2'-amino-5'-chloro-phenyl) -3-furan-3-yl-1H-1,2,4-triazole, n = 1; L4 = 3-adamantane-1-yl-5- (2'-amino-phenyl) -1H-1,2 4-triazole, n = 2; L5 = 5- (2'-amino-3'-methyl-phenyl) -3-furan-3-yl-1H-1,2,4-triazole, n = 1; L6 = 3-thiophene-3-yl-5- (2'-amino-3'-fluoro-phenyl) -1H-1,2,4-triazole, n = 2; L7 = 3-thiophene-2-yl-5 - (2'-amino-3'-fluoro-phenyl) -1H-1,2,4-triazole, n = 3). Working 1×10^{-4 M}aqueous salt solutions were prepared in a plastic container. Determination of the soluble form of silica products of hydrolysis hexafluorosilicates conducted photocolorimetric method. The measurement was performed at a wavelength of 380 nm.

Results and discussion

         We found a general tendency to reduce the values of α for hexafluorosilicates 1,2,4-triazole compared with pyridinium salts, which is close to the degree of hydrolysis quantity. In the case of salts of 1,2,4-triazole less efficient release of fluoride ions by hydrolysis circuits may be accompanied by a decrease caries-preventive effect of the studied compounds. During the preparation 1×10^{-4 M} salt solutions in all cases observed precipitate soluble free base L by hydrolysis in cation. For a given concentration of solutions villages are not subjected to further dissolution prolonged aging, to evaluate the upper limit of solubility of salts of 1,2,4-triazole in ≤ 0.0002 mol. %. Very low solubility studied in this paper salts of 3,5-disubstituted 1,2,4-triazole derivatives and 3,5-diamino-1,2,4-triazole related obviously dominated lipophilic contribution to the hydrophilic-lipophilic balance heterocyclic bases L1 - L7.

Conclusions

         Estimated value of solubility hexafluorosilicates 3,5-disubstituted 1,2,4-triazole derivatives in water in the lowest number of similar salts of heterocyclic cations. The degree of hydrolysis of 1,2,4-triazole hexafluorosilicates in aqueous solution by an average of 10 - 30% lower compared with the corresponding values for pyridinium salts. The experimental and calculated data do not consider hexafluorosilicates 3,5-disubstituted 1,2,4-triazole derivatives as promising caries-preventive agents.