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Synthesis and Cardiotropic Activity of Linear Methoxyphenyltriazaalkanes

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Pharmaceutical Chemistry Journal Aims and scope

A new group of potential pFOX inhibitors among linear methoxyphenyltriazaalkanes were designed and synthesized. Cardiotropic activity in rodent experiments was found for most of the synthesized compounds. The most active compound N1-(2,3,4-trimethoxybenzyl)-N2-{2-[(2,3,4-trimethoxybenzyl)amino]ethyl}-1,2-ethanediamine trihydrochloride (LM-1) combined anti-ischemic, antiarrhythmic, and antifibrillatory activities (1 mg/kg, i.v.) and low toxicity (LD50 = 119 mg/kg, mice, i.p.) and was selected for development as a potential cardiotropic drug.

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References

  1. L. M. McComick, A. C. Kydd, and D. P. Dutka, Cardiovasc. Hematol. Agents Med. Chem., 10(4), 319 – 324 (2012).

    Article  Google Scholar 

  2. A. N. Grossman, L. H. Opie, J. R. Beshansky, et al., Circulation, 127(9), 1040 – 1048 (2013).

    Article  Google Scholar 

  3. V. M. Olesova, O. Yu. Markatyuk, Yu. Yu. Yurova, and A. G. Obrezan, Kardiologiya, 53(1), 66 – 71 (2013).

    CAS  PubMed  Google Scholar 

  4. G. D. Lopaschuk, J. R. Ussher, C. D Folmes, et al., Physiol. Rev., 90(1), 207 – 258 (2010).

    Article  CAS  Google Scholar 

  5. V. Lionetti, W. C. Stanley, and F. A. Recchia, Cardiovasc. Res., 90(2), 202 – 209 (2011).

    Article  CAS  Google Scholar 

  6. J. S. Jaswal, W. Keung, W. Wang, et al., Biochim. Biophys. Acta, 1813(7), 1333 – 1350 (2011).

    Article  CAS  Google Scholar 

  7. J. S. Ingwall, Cardiovasc. Res., 81(3), 412 – 419 (2009).

    Article  CAS  Google Scholar 

  8. M. van Bilsen, P. J. H. Smeets, A. J. Gilde, and G. J. van der Vusse, Cardiovasc. Res., 61(2), 218 – 226 (2004).

    Article  Google Scholar 

  9. B. Bhandari and L. Subramanian, Recent Pat. Cardiovasc. Drug Discovery, 2(1), 35 – 39 (2007).

    Article  CAS  Google Scholar 

  10. Y. H. Fang, L. Piao, Z. Hong, et al., J. Mol. Med. (Berlin), 90(1), 31 – 43 (2012).

    Article  CAS  Google Scholar 

  11. P. F. Kantor, A. Lucien, R. Kozak, and G. D. Lopaschuk, Circ. Res., 86(5), 580 – 588 (2000).

    Article  CAS  Google Scholar 

  12. M. Aldakkak, A. K. Camara, J. S. Heisner, et al., Pharmacol. Res., 64(4), 381 – 392 (2011).

    Article  CAS  Google Scholar 

  13. K. M. Wyatt, C. Skene, K. Veitch, et al., Biochem. Pharmacol., 50(10), 1599 – 1606 (1995).

    Article  CAS  Google Scholar 

  14. M. Imai, S. Rastogi, N. Sharma, et al., Cardiovasc. Drugs Ther., 21(1), 9 – 15 (2007).

    Article  CAS  Google Scholar 

  15. P. Partownavid, S. Umar, J. Li, et al., Crit. Care Med., 40(8), 2431 – 2437 (2012).

    Article  CAS  Google Scholar 

  16. G. Fragasso, A. Salerno, R. Spoladore, et al., Curr. Pharm. Des., 15(8), 857 – 862 (2009).

    Article  CAS  Google Scholar 

  17. B. Hu, W. Li, T. Xu, et al., Clin. Cardiol., 34(6), 395 – 400 (2011).

    Article  Google Scholar 

  18. L. Zhang, Y. Lu, H. Jiang, et al., J. Am. Coll. Cardiol., 59(10), 913 – 922 (2012).

    Article  CAS  Google Scholar 

  19. E. Vizzardi, A. D’Aloia, F. Quinzani, et al., J. Cardiovasc. Pharmacol. Ther., 17(4), 353 – 356 (2012).

    Article  CAS  Google Scholar 

  20. S. Sossalla and L. S. Maier, Pharmacol. Ther., 133(3), 311 – 323 (2012).

    Article  CAS  Google Scholar 

  21. S. Yamamoto, K. Matsui, M. Sasabe, and N. Ohashi, J. Cardiovasc. Pharmacol., 39(2), 234 – 241 (2002).

    CAS  Google Scholar 

  22. A. N. Mironov, Handbook for Preclinical Drug Trials [in Russian], Part 1, Grif i K, Moscow, 2013, pp. 385 – 416.

  23. I. A. Ilyushkina, A. N. Berchatova, I. A. D’yachenko, et al., Biomeditsina, No. 2, 6 – 13 (2012).

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Correspondence to G. V. Mokrov.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 53, No. 6, pp. 16 – 23, June, 2019.

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Mokrov, G.V., Likhosherstov, A.M., Barchukov, V.V. et al. Synthesis and Cardiotropic Activity of Linear Methoxyphenyltriazaalkanes. Pharm Chem J 53, 500–506 (2019). https://doi.org/10.1007/s11094-019-02027-7

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  • DOI: https://doi.org/10.1007/s11094-019-02027-7

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