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Synthesis and Study of New Anticoagulant Candidates Based on 6-Aryl-5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinoline-1,2-diones
Russian Journal of General Chemistry ( IF 0.9 ) Pub Date : 2023-12-07 , DOI: 10.1134/s1070363223140359 A. A. Skoptsova , N. P. Novichikhina , E. A. Kosheleva , S. V. Baranin , N. A. Podoplelova , M. A. Panteleev , Kh. S. Shikhaliev
中文翻译:
6-芳基-5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1,2-二酮类新型抗凝剂的合成与研究
更新日期:2023-12-07
Russian Journal of General Chemistry ( IF 0.9 ) Pub Date : 2023-12-07 , DOI: 10.1134/s1070363223140359 A. A. Skoptsova , N. P. Novichikhina , E. A. Kosheleva , S. V. Baranin , N. A. Podoplelova , M. A. Panteleev , Kh. S. Shikhaliev
Abstract
ction 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.
中文翻译:
6-芳基-5,6-二氢-4H-吡咯并[3,2,1-ij]喹啉-1,2-二酮类新型抗凝剂的合成与研究
摘要
6-芳基-5,6-二氢-4 H-吡咯并[3,2,1- ij ]喹啉-1,2-二酮与3-乙酰香豆素的反应导致形成一系列新的1-[2-氧代-2-(2-氧代-2H-苯并-3-基)亚乙基]-6-芳基-5,6-二氢-4H-吡咯并[3,2,1- ij ]喹啉-2( 1H)-那些。对所有目标化合物进行针对凝血因子 Xa 和 XIa 的抗凝血活性的初步体外筛选。还测定了合成分子中显示最高抑制值的结构的IC 50值。