☆ 4.2 Article

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

PHARMACEUTICAL CHEMISTRY JOURNAL (2018)

期刊

PHARMACEUTICAL CHEMISTRY JOURNAL

卷 51, 期 11, 页码 975-979

出版社

SPRINGER

DOI: 10.1007/s11094-018-1726-4

关键词

pyrrolo[3,2,1-ij]quinolin-2-ones; derivatives; condensation; molecular docking; factor-Xa inhibitors; anticoagulants

类别

Chemistry, Medicinal Pharmacology & Pharmacy

资金

FTP [14.577.21.0182, RFMEFI57715X0182]
RSF [14 - 50 - 00029]

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摘要

New factor-Xa inhibitors in a series of pyrrolo[3,2,1-ij]quinoline-1,2-diones substituted by condensation at the beta-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 mu M) were discovered.

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