Synthesis, Docking, and Anticoagulant Activity of New Factor-Xa Inhibitors in a Series of Pyrrolo[3,2,1-ij]Quinoline-1,2-Diones
- Authors: Medvedeva S.M.1, Potapov A.Y.1, Gribkova I.V.2, Katkova E.V.3, Sulimov V.B.2, Shikhaliev K.S.3
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Affiliations:
- Voronezh State University
- Federal Hematological Research Center, Ministry of Health of the Russian Federation
- Research Computing Centre, M. V. Lomonosov Moscow State University
- Issue: Vol 51, No 11 (2018)
- Pages: 975-979
- Section: Article
- URL: https://journals.rcsi.science/0091-150X/article/view/244877
- DOI: https://doi.org/10.1007/s11094-018-1726-4
- ID: 244877
Cite item
Abstract
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.
About the authors
S. M. Medvedeva
Voronezh State University
Author for correspondence.
Email: SMMedvedeva@rambler.ru
Russian Federation, 1 Universitetskaya Sq, Voronezh, 394006
A. Yu. Potapov
Voronezh State University
Email: SMMedvedeva@rambler.ru
Russian Federation, 1 Universitetskaya Sq, Voronezh, 394006
I. V. Gribkova
Federal Hematological Research Center, Ministry of Health of the Russian Federation
Email: SMMedvedeva@rambler.ru
Russian Federation, 4 Novyi Zykovskii Proezd, Moscow, 125167
E. V. Katkova
Research Computing Centre, M. V. Lomonosov Moscow State University
Email: SMMedvedeva@rambler.ru
Russian Federation, 1/4 Leninskie Gory, Moscow, 119991
V. B. Sulimov
Federal Hematological Research Center, Ministry of Health of the Russian Federation
Email: SMMedvedeva@rambler.ru
Russian Federation, 4 Novyi Zykovskii Proezd, Moscow, 125167
Kh. S. Shikhaliev
Research Computing Centre, M. V. Lomonosov Moscow State University
Email: SMMedvedeva@rambler.ru
Russian Federation, 1/4 Leninskie Gory, Moscow, 119991