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 |
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container_title | Pharmaceutical chemistry journal |
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creator | Medvedeva, S. M. Potapov, A. Yu Gribkova, I. V. Katkova, E. V. Sulimov, V. B. Shikhaliev, Kh. S. |
description | 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. |
doi_str_mv | 10.1007/s11094-018-1726-4 |
format | Article |
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ij
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H
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subjects | Alkaloids Anticoagulants Medicine Organic Chemistry Pharmacology/Toxicology Pharmacy Quinoline Thrombin |
title | 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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