Synthesis and structure–activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells
摘要:
A series of diarylamide derivatives were synthesized and evaluated for their inhibitory activities against human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs). Compound 2w was superior to the lead compound, Tranilast, in terms of the potency of the activity and cell selectivity. (C) 2001 Elsevier Science Ltd. All rights reserved.
Synthesis and structure–activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells
摘要:
A series of diarylamide derivatives were synthesized and evaluated for their inhibitory activities against human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs). Compound 2w was superior to the lead compound, Tranilast, in terms of the potency of the activity and cell selectivity. (C) 2001 Elsevier Science Ltd. All rights reserved.
Abstract Herein we report a robust and synthetically useful catalyst-free amination methodology by the coupling of carboxylic acids and N-substituted formamides using POCl3 as a promoter. Versatile amides with a wide array of substituent groups were prepared within only 1 h in good to excellent yields. And even multi-substituted aromatic carboxylic acids could give the desired products with satisfactory
摘要在此我们报告了一种稳健且合成有用的无催化剂胺化方法,该方法通过使用 POCl3 作为促进剂将羧酸和 N 取代甲酰胺偶联。具有多种取代基的多功能酰胺仅在 1 小时内就以良好到极好的收率制备。甚至多取代的芳族羧酸也可以得到令人满意的结果。图形概要
Synthesis and structure–activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells
A series of diarylamide derivatives were synthesized and evaluated for their inhibitory activities against human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs). Compound 2w was superior to the lead compound, Tranilast, in terms of the potency of the activity and cell selectivity. (C) 2001 Elsevier Science Ltd. All rights reserved.