Synthesis and Study of New Anticoagulant Candidates Based on 6-Aryl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline-1,2-diones

被引：1

作者：

Skoptsova, A. A. ^{[1
]}

Novichikhina, N. P. ^{[1
]}

Kosheleva, E. A. ^{[1
]}

Baranin, S. V. ^{[2
]}

Podoplelova, N. A. ^{[3
]}

Panteleev, M. A. ^{[3
]}

Shikhaliev, Kh. S. ^{[1
]}

机构：

[1] Voronezh State Univ, Voronezh 394018, Russia

[2] Russian Acad Sci, ND Zelinsky Inst Organ Chem, Moscow 119991, Russia

[3] Russian Acad Sci, Ctr Theoret Problems Physico Chem Pharmacol, Moscow 109029, Russia

来源：

RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2023年 / 93卷 / SUPPL 1期

关键词：

4H-pyrrolo[3,2,1-ij]quinoline-1,2-dione; 3-acetylcoumarin; anticoagulant activity; inhibition; factor Xa; factor XIa; BIOLOGICAL EVALUATION; FACTOR-XA; DESIGN; INHIBITORS; ANTIBACTERIAL; DERIVATIVES; FRAGMENT; HYBRID; AGENTS;

D O I：

10.1134/S1070363223140359

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The reaction of 6-aryl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline-1,2-diones with 3-acetylcoumarins led to the formation of a new series of 1-[2-oxo-2-(2-oxo-2H-chromen-3-yl)ethylidene]-6-aryl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline-2(1H)-ones. Primary in vitro screening of anticoagulant activity against coagulation factors Xa and XIa was performed for all target compounds. The IC50 value was also determined for the structures that showed the highest inhibition values among synthesized molecules.

引用

页码：S115 / S123

页数：9

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