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Antiarrhythmic, Hemostatic, Anthelmintic, and Larvicidal Activity of 3,3-Dialkyl-Substituted Drotaverine Analogs
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2021-08-13 , DOI: 10.1007/s11094-021-02438-5
A. G. Mikhailovskii 1 , E. S. Pogorelova 1 , I. P. Rudakova 1 , A. V. Starkova 1 , N. N. Pershina 1
Affiliation  

Previously obtained hydrochlorides of 1-[3,4-(R1)2-benzyl]-3,3-(R2)2-6,7-(R3)2-3,4-dihydroisoquinolines (R1 = H, MeO, EtO; R2 = Alk; R3 = MeO, EtO) and their benzo[f]-analogs proved to be water-soluble compounds. This advantage enabled additional biological testing of them for a number of activity types such as antiarrhythmic, hemostatic, anthelmintic, and larvicidal. All isoquinoline hydrochlorides were tested for antiarrhythmic activity (CaCl2 model) with 7 of 13 compounds being active. The maximum antiarrhythmic index was 3.97. The obtained isoquinolines were predominantly coagulants (hemostatics) with respect to blood clotting. The most active compound increased blood coagulation by 46.6%. All compounds with anthelmintic activity exceeded the effect of pyrantel. The larvicidal (insecticidal) effect of the most active compound was comparable with that of diazinon.



中文翻译:

3,3-二烷基取代的屈他维林类似物的抗心律失常、止血、驱虫和杀幼虫活性

先前获得的 1-[3,4-(R 1 ) 2 -苄基]-3,3-(R 2 ) 2 -6,7-(R 3 ) 2 -3,4-二氢异喹啉的盐酸盐(R 1 = H , MeO, EtO; R 2 = Alk; R 3 = MeO, EtO) 和它们的苯并[ f ]-类似物被证明是水溶性化合物。这一优势使得可以对它们的多种活性类型进行额外的生物测试,例如抗心律失常、止血、驱虫和杀幼虫。测试了所有异喹啉盐酸盐的抗心律失常活性 (CaCl 2模型),其中 13 种化合物中有 7 种具有活性。最大抗心律失常指数为 3.97。获得的异喹啉在凝血方面主要是凝血剂(止血剂)。最活跃的化合物使血液凝固增加了 46.6%。所有具有驱虫活性的化合物都超过了吡喃特的作用。最活性化合物的杀幼虫(杀虫)效果与二嗪农相当。

更新日期:2021-08-19
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