Parenti C, Di Bella M, Raffa L, Baggio G G, Guarini S
Farmaco Sci. 1983 Oct;38(10):738-49.
A series of quaternary ammonium salts of 3-alkylaminoderivatives of 1,2,4-benzothiadiazine-1,1-dioxide were prepared and tested for cardiovascular activity. Almost all the substances tested proved to have some measure of depressant activity on arterial pressure and the most interesting compounds in this respect were (XII), (XIII), (XV) and (XIX) for which hypotensive values between 60 and 70% with respect to the base level were recorded. Compound (XV) also caused increase in the differential pressure and decrease of cardiac frequency. The later however was increased by some other compounds [(XII), (XVIII)]. The structure-activity relationships are discussed taking into account also the activity of the parent tertiary amines.
制备了一系列1,2,4-苯并噻二嗪-1,1-二氧化物的3-烷基氨基衍生物的季铵盐,并测试了它们的心血管活性。几乎所有测试的物质都被证明对动脉血压有一定程度的抑制活性,在这方面最有趣的化合物是(XII)、(XIII)、(XV)和(XIX),记录到它们相对于基线水平的降压值在60%至70%之间。化合物(XV)还导致压差增加和心率降低。然而,其他一些化合物[(XII)、(XVIII)]使心率增加。还考虑了母体叔胺的活性来讨论构效关系。