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

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

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...

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Veröffentlicht in:Pharmaceutical chemistry journal 2018-02, Vol.51 (11), p.975-979
Hauptverfasser: Medvedeva, S. M., Potapov, A. Yu, Gribkova, I. V., Katkova, E. V., Sulimov, V. B., Shikhaliev, Kh. S.
Format: Artikel
Sprache:eng
Schlagworte:
Alkaloids
Anticoagulants
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Quinoline
Thrombin
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Zusammenfassung: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 (IC 50 = 0.7 – 40 μM) were discovered.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-018-1726-4