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Antiarrhythmic, Hemostatic, Anthelmintic, and Larvicidal Activity of 3,3-Dialkyl-Substituted Drotaverine Analogs

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Pharmaceutical Chemistry Journal Aims and scope

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.

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Authors and Affiliations

  1. Perm State Pharmaceutical Academy, Ministry of Health of the Russian Federation, 2 Polevaya St., Perm, 614990, Russia

    A. G. Mikhailovskii, E. S. Pogorelova, I. P. Rudakova, A. V. Starkova & N. N. Pershina

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  1. A. G. Mikhailovskii
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  2. E. S. Pogorelova
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  3. I. P. Rudakova
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  4. A. V. Starkova
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  5. N. N. Pershina
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Correspondence to A. G. Mikhailovskii.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 55, No. 5, pp. 9 – 12, May, 2021.

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Mikhailovskii, A.G., Pogorelova, E.S., Rudakova, I.P. et al. Antiarrhythmic, Hemostatic, Anthelmintic, and Larvicidal Activity of 3,3-Dialkyl-Substituted Drotaverine Analogs. Pharm Chem J 55, 423–426 (2021). https://doi.org/10.1007/s11094-021-02438-5

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  • DOI: https://doi.org/10.1007/s11094-021-02438-5

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