期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 24, 页码 6919-6923出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.10.015
关键词
Ischemic cerebrovascular disease; Thrombin; Antioxidant; Solubility; Scutellarin; Scutellarein
资金
- National Natural Science Foundation of China [81001382, 81274058]
- Ministry of Education [NCET-09-0163]
- 333 High-level Talents Training Project
- Jiangsu Province [2011-D-078]
- Six Talents Project
- Program for Outstanding Scientific and Technological Innovation Team of Jiangsu Higher Education
- National Key Technology RD Program [2008BAI51B01]
- Key Research Project in Basic Science of Jiangsu College and University [07KJA36024, 10KJA360039]
- Priority Academic Program Development of Jiangsu Higher Education Institutions [ysxk-2010]
- Construction Project for Jiangsu Engineering Center of Innovative Drug from Blood-conditioning TCM Formulae
Two series of 8-aminomethylated derivatives were prepared by Mannich reaction of scutellarein (2) with appropriate aliphatic amines, alicyclic amines and formaldehyde. All the compounds were tested for their thrombin inhibition activity through the analyzation of prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT) and fibrinogen (FIB). The antioxidant activities of these target products were assessed by 1,1-diphenyl-2-picrylhydrazyl radical 2,2-diphenyl-1-(2,4,6-trinitrophenyl) hydrazyl (DPPH) assay using 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide (MTT) assay method and the solubility were assessed by ultraviolet (UV). The results showed that morpholinyl aminomethylene substituent derivative (3d) demonstrated stronger anticoagulant activity, better water solubility and good antioxidant activity compared with scutellarein (2), which warrants further development as a agent for ischemic cerebrovascular disease treatment. (C) 2012 Elsevier Ltd. All rights reserved.
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