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Synthesis and Cardiotropic Activity of N,N′-Diarylpropane-1,3-Diamines

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Pharmaceutical Chemistry Journal Aims and scope

We report here the synthesis of novel compounds of the bis-(2,3,4-trimethoxybenzyl)propanediamines group and studies of their anti-ischemic and antiarrhythmic activity. Introduction of a hydroxyl group into the central part of the propane linker was found to produce virtually no change in the spectrum of cardiotropic properties of the unsubstituted compound ALM-851, while introduction of two methyl groups led to the complete disappearance of both antiarrhythmic and antiischemic activities. Compound ALM-850 (1,3-bis((2,3,4-trimethoxy-benzyl)amino)propan-2-oldihydrochloride) at a dose of 3 mg/kg significantly blocked the development of rhythm disturbances and death in animals in the aconitine and calcium chloride arrhythmia models, and also decreased ST segment depression in the isoproterenol ischemia model.

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Authors and Affiliations

  1. V. V. Zakusov Science Research Institute of Pharmacology, 8 Baltiiskaya Street, 125315, Moscow, Russia

    G. V. Mokrov, T. Yu. Vorob’eva, V. E. Biryukova, E. I. Barchukova, V. V. Barchukov, I. B. Tsorin, M. B. Vititnova, A. G. Rebeko & S. A. Kryzhanovskii

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  1. G. V. Mokrov
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  2. T. Yu. Vorob’eva
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  3. V. E. Biryukova
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  4. E. I. Barchukova
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  5. V. V. Barchukov
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  6. I. B. Tsorin
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  7. M. B. Vititnova
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  8. A. G. Rebeko
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  9. S. A. Kryzhanovskii
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Corresponding author

Correspondence to G. V. Mokrov.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 57, No. 7, pp. 7 – 12, July, 2023.

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Mokrov, G.V., Vorob’eva, T.Y., Biryukova, V.E. et al. Synthesis and Cardiotropic Activity of N,N′-Diarylpropane-1,3-Diamines. Pharm Chem J 57, 975–980 (2023). https://doi.org/10.1007/s11094-023-02973-3

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  • DOI: https://doi.org/10.1007/s11094-023-02973-3

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