Bernabei M T, Cameroni R, Forni F, Bellei S, Baggio G
Farmaco Sci. 1978 Oct;33(10):791-8.
A series of 4-dimethylaminoethyl and 4-diethylaminoethyl derivatives of 2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c] [1,2,4] benzothiadiazine-5,5-dioxide substituted or unsubstituted in the benzene ring was prepared and subjected to preliminary investigation using the cardiovascular system of the anesthesized rat. Introduction of a basic group in the alkyl chain on N4 gives compounds with good hypotensive activity, this being most pronounced for (III, IV a and XIV) and an increase in differential pressure, marked for (V a, X, XII). These effects are sometimes accompanied by some bradycardizing activity, most marked for (V a) and (X). The results therefore confirm that derivatives of tetrahydropyrrolbenzothiazine have cardiovascular activity. Structure-activity relationships are discussed.
制备了一系列在苯环上被取代或未被取代的2,3,3a,4-四氢-1H-吡咯并[2,1-c][1,2,4]苯并噻二嗪-5,5-二氧化物的4-二甲基氨基乙基和4-二乙氨基乙基衍生物,并利用麻醉大鼠的心血管系统进行了初步研究。在N4的烷基链中引入碱性基团可得到具有良好降压活性的化合物,这在(III、IV a和XIV)中最为明显,而压差增加在(V a、X、XII)中较为显著。这些作用有时会伴有一些心动过缓活性,在(V a)和(X)中最为明显。因此,结果证实了四氢吡咯苯并噻嗪衍生物具有心血管活性。讨论了构效关系。