Design,synthesis of novel quinazolinon compounds as human anti-acrosin inhibitor
- Received Date: 2010-01-19
- Rev Recd Date: 2010-03-09
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Key words:
- acrosin inhibitor /
- design /
- synthesis /
- anti-acrosin activity /
- quinazolinon /
Abstract: Objective Novel 3-substituted quinazolinon compounds were designed and synthesised on the base of the active site of human acrosin. Methods The compounds were designed by computer and chemically synthesised. Results Seven 3-substituted quinazolinon compounds were designed and synthesised,subsequently carried out in vitro anti-acrosin test. Conclusion The Results of anti-acrosin tese in vitro exhibited that all the compounds showed potent anti-acrosin activities.Particularly,compounds 3 g displayed much stronger anti-acrosin activities(229 times) than that of TLCK.
Citation: | NING Wei-wei, LIU Xue-fei, ZHANG Xiao-meng, ZHENG Can-hui, SHENG Chun-quan, ZHOU You-jun, ZHANG Ling, LV Jia-guo, ZHU Ju. Design,synthesis of novel quinazolinon compounds as human anti-acrosin inhibitor[J]. Journal of Pharmaceutical Practice and Service, 2010, 28(4): 296-298,312. |