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Synthesis, Docking, and Anticoagulant Activity of New Factor-Xa Inhibitors in a Series of Pyrrolo[3,2,1-ij]Quinoline-1,2-Diones

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Pharmaceutical Chemistry Journal Aims and scope

New factor-Xa inhibitors in a series of pyrrolo[3,2,1-ij]quinoline-1,2-diones substituted by condensation at the β-carbonyl with rhodanine, arylamines, and H-tryptamines were synthesized, characterized, and studied by molecular docking. Promising factor-Xa inhibitors with inhibitory constants in the micromolar concentration range (IC50 = 0.7 – 40 μM) were discovered.

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Acknowledgments

New compounds were synthesized with support of the FTP “Research and development in priority directions for development of the Russian science and technology complex for 2014 – 2020 (Contract No. 14.577.21.0182, unique identifier of applied scientific research RFMEFI57715X0182). Molecular docking and post-processing studies for discovering and designing new inhibitors were supported by RSF Grant 14 – 50 – 00029.

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Authors and Affiliations

  1. Voronezh State University, 1 Universitetskaya Sq, Voronezh, 394006, Russia

    S. M. Medvedeva & A. Yu. Potapov

  2. Federal Hematological Research Center, Ministry of Health of the Russian Federation, 4 Novyi Zykovskii Proezd, Moscow, 125167, Russia

    I. V. Gribkova & V. B. Sulimov

  3. Research Computing Centre, M. V. Lomonosov Moscow State University, 1/4 Leninskie Gory, Moscow, 119991, Russia

    E. V. Katkova & Kh. S. Shikhaliev

Authors
  1. S. M. Medvedeva
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  2. A. Yu. Potapov
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  3. I. V. Gribkova
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  4. E. V. Katkova
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  5. V. B. Sulimov
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  6. Kh. S. Shikhaliev
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Corresponding author

Correspondence to S. M. Medvedeva.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 51, No. 11, pp. 19 – 23, November, 2017.

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Medvedeva, S.M., Potapov, A.Y., Gribkova, I.V. et al. Synthesis, Docking, and Anticoagulant Activity of New Factor-Xa Inhibitors in a Series of Pyrrolo[3,2,1-ij]Quinoline-1,2-Diones. Pharm Chem J 51, 975–979 (2018). https://doi.org/10.1007/s11094-018-1726-4

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  • DOI: https://doi.org/10.1007/s11094-018-1726-4

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