Cameroni R, Bernabei M T, Forni F, Baggio G
Farmaco Sci. 1978 Sep;33(9):713-20.
A series of 4-propylderivatives of 2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c] [1,2,4]benzothiadizine-5,5-dioxide substituted or unsubstituted in the benzene ring was synthesized. Derivatives of these compounds together with those of the corresponding 4-methyl and 4-ethyl derivatives prepared previously were tested for cardiovascular effects in the anesthesized rat. All the compounds studied showed hypotensive activity which was particularly intense for compounds (X), (XIX), (XXII), (XXV), and produced an increase in differential pressure marked for (XXV) and (XXVIII) which was often accompanied by pronounced bradycardia (XVII), (XVIII) and (XIX). The results prove that derivatives of 2,3,3a,4-tetrahydro-1H-pyrrolo-[2,1-c][1,2,4]benzothiadiazine-5,5-dioxide have hypotensive and bradycardizing activity. Structure-activity relationships are discussed.
合成了一系列苯环上有取代或无取代的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-丙基衍生物。将这些化合物的衍生物与先前制备的相应4-甲基和4-乙基衍生物的衍生物一起在麻醉大鼠中测试其心血管效应。所有研究的化合物均显示出降压活性,其中化合物(X)、(XIX)、(XXII)、(XXV)的降压活性尤为强烈,并且化合物(XXV)和(XXVIII)使压差增加明显,这常常伴有明显的心动过缓(如(XVII)、(XVIII)和(XIX))。结果证明2,3,3a,4-四氢-1H-吡咯并[2,1-c][1,2,4]苯并噻二嗪-5,5-二氧化物的衍生物具有降压和致心动过缓活性。讨论了构效关系。