Monzani A, di Bella M, Ferrari P, Parenti C, Raffa L
Farmaco Sci. 1979 Oct;34(10):876-83.
A series of carboxy- and carbomethoxyalkyl derivatives of 3-amino-1,2,4-benzothiaidazin-1,1-dioxide either substituted or unsubstituted in the benzene ring [compounds (I leads to XVIII)] was prepared and tested for cardiovascular activity. It was found that the introduction of a carboxy-or carbalkoxy-group in the omega position of 3-alkylamino derivatives of 1,2,4-benzothiadiazine-1,1-dioxide usually causes marked decrease or abolition of the cardiovascular activity shown by the parent compounds. The negative effect on the pressor trace (hypotension and increase in differential pressure) is more frequent and significant than that on bradycardial activity.
制备了一系列苯环上有取代或无取代的 3-氨基-1,2,4-苯并噻二嗪-1,1-二氧化物的羧基和甲氧基烷基衍生物(化合物(I至XVIII)),并对其心血管活性进行了测试。结果发现,在1,2,4-苯并噻二嗪-1,1-二氧化物的3-烷基氨基衍生物的ω位引入羧基或烷氧基通常会导致母体化合物所显示的心血管活性显著降低或丧失。对升压曲线(低血压和压差增加)的负面影响比对心动过缓活性的影响更频繁且更显著。