|
|
|
| Synthesis and Anticoagulant Activities of Novel Benzimidazole Derivatives |
| CAI Zhi-qiang, HOU Xu, ZHANG Bo, LIU Ruo-can |
| School of Petrochemical Engineering, Shenyang University of Technology, Liaoyang 111003, China |
|
|
|
|
Abstract Ethyl 3-｛2-［(4-cyano-3-fluorophenyl substituent)methyl］-1-methyl-N-(pyridin-2-yl)-1H-benzo［d］imidazole-5-carboxamido｝propanoate（3a，3e） were prepared by cyclization of ethyl-3-［3-amino-4-(methylamino)-N-(pyridin-2-yl)benzamido］propanoate with 2-(4-cyano-3-fluorophenyl substituent)acetic acid． 2-{3-［2-(4-Cyano-3-fluorophenyl substituent)methyl］-1-methyl-N-(pyridin-2-yl)-1H-benzo［d］imidazole-5-carboxamido｝propanamido substituent（6a~6h） were prepared by hydrolysis and amidation from 3． Eight novel benzoimidazole derivatives（7a~7h） were synthesized by cyclization reaction of 6 with acetomenadione． The structures were characterized by 1H NMR and HR-ESI-MS. The anticoagulant activities of 7a~7h were investigated. The results showed that 7a and 7c exhibited anticoagulant activities. The aPTTs were （83.1±4.2）s and （80.7±2.9）s, respectively, which were better than dabigatran etexilate（75.3±2.1）s.
|
|
Received: 09 April 2015
|
|
|
|
|
|
|
2015, Vol. 23 
