Mannich bases of scutellarein as thrombin-inhibitors: Design,synthesis, biological activity and solubility |
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Authors: | Nian-Guang Li Shu-Lin Song Min-Zhe Shen Yu-Ping Tang Zhi-Hao Shi Hao Tang Qian-Ping Shi Yi-Fan Fu Jian-Ao Duan |
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Institution: | 1. Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China;2. Department of Medicinal Chemistry, Nanjing University of Chinese Medicine, Nanjing 210046, China;3. Department of Organic Chemistry, China Pharmaceutical University, Nanjing 211198, China |
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Abstract: | 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. |
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