谢毓元, 徐杰诚, 嵇汝运. 几种药用锑制剂的锡相应化合物J. 药学学报, 1957, 5(2): 123-128.
引用本文: 谢毓元, 徐杰诚, 嵇汝运. 几种药用锑制剂的锡相应化合物J. 药学学报, 1957, 5(2): 123-128.
HSIEH YU-YUAN, HSU JE-ZEN AND KYI ZU-YOONG, . TIN ANALOGUES OF SOME THERAPEUTIC ANTIMONIALSJ. Acta Pharmaceutica Sinica, 1957, 5(2): 123-128.
Citation: HSIEH YU-YUAN, HSU JE-ZEN AND KYI ZU-YOONG, . TIN ANALOGUES OF SOME THERAPEUTIC ANTIMONIALSJ. Acta Pharmaceutica Sinica, 1957, 5(2): 123-128.

几种药用锑制剂的锡相应化合物

TIN ANALOGUES OF SOME THERAPEUTIC ANTIMONIALS

  • Abstract: Organoantimony derivatives have been widely used for the treatment of schis- tosomiasis, leishmaniasis and filariasis. These drugs, however, suffer from a low margin of safety. Attempts are, therefore, made to prepare the tin analogues of tartar emetic (potassium antimonyl tartrate) (Ⅰ), n-butyl antimonylgallate (Ⅱ) and Fuadin (Ⅲ) in order to search for less toxic chemotherapeutic agents. Treatment of ammonium tartrate with stannous chloride and stannic oxide gave 4,5-dicarboxyl-4,5-dihydro-l,3-dioxastanniol(IV)and 4,5-dicarboxyl-4,5-dihydro-2-oxo- 1,3-dioxastanniol diammonium salt (V) respectively. n-Butyl stannylgallate (Ⅵ) was resulted on interaction of n-butyl gallate with stannous chloride. Stannous and stannic bis-(1,2-dihydroxyl-3,5-dipotassium disulphonate) were afforded by potas- sium catechol-3,5-disulphonate. The therapeutic value of p-carboxyphenoxymethyl-4,5-dihydro-l,3-dithiastibiol (Ⅸ) was indicated in our previous work, the corresponding cyclic stannous (Ⅹ) and stannic (Ⅺ) mercaptides were now prepared on treatment of p-carboxyphenyl dimercaptopropyl ether with stannous and stannic chloride respectively. The organotin derivatives so prepared were used for treatment of mice in- fected with Schistosomiasis japonica. The stannous compounds were more active than the stannic analogues. Compounds VI and X had therapeutic ratios as favourable as tartar emetic.

     

/

返回文章
返回