FAN Yong-zheng, CHEN Qian-qian, LIU Bo-shi, ZHAO Jun-tao, TIAN Wei, ZHOU You-jun, LV Jia-guo, ZHU Ju. Synthesis and effect of novel 1-(1H-benzimidazole-2-yl) -urea derivatives as human acrosin inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(3): 203-206,210. doi: 10.3969/j.issn.1006-0111.2012.03.012
| Citation:
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FAN Yong-zheng, CHEN Qian-qian, LIU Bo-shi, ZHAO Jun-tao, TIAN Wei, ZHOU You-jun, LV Jia-guo, ZHU Ju. Synthesis and effect of novel 1-(1H-benzimidazole-2-yl) -urea derivatives as human acrosin inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(3): 203-206,210. doi: 10.3969/j.issn.1006-0111.2012.03.012
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Synthesis and effect of novel 1-(1H-benzimidazole-2-yl) -urea derivatives as human acrosin inhibitors
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Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
- Received Date: 2012-02-13
- Rev Recd Date:
2012-03-27
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Abstract
Objective To design and synthesize novel 1-(1H-benzimidazole-2-yl)urea compounds on the basis of the active site of human acrosin. Methods The compounds were designed by computer modeling and synthesized. Results Ten 1-(1H-benzimidazole-2-yl)urea compounds were designed and synthesized, in vitro anti-acrosin activity were tested. Conclusions The results of in vitro anti-acrosin test showed that all the compounds had better acrosin inhibitory activity than that of the control compound TLCK.Among them compound 8a was the most potent one, with IC50 0.098 9 mmol/L.
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