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ZHAO Fang-zhen, ZHUANG Chun-lin, GUO Zi-zhao, SHENG Chun-quan, YAO Jian-zhong, MIAO Zhen-yuan, ZHANG Wan-nian. Synthesis and biological activity of 1H-pyrrol-2(5H)-ones[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(6): 430-432,456. doi: 10.3969/j.issn.1006-0111.2012.06.009
Citation: ZHAO Fang-zhen, ZHUANG Chun-lin, GUO Zi-zhao, SHENG Chun-quan, YAO Jian-zhong, MIAO Zhen-yuan, ZHANG Wan-nian. Synthesis and biological activity of 1H-pyrrol-2(5H)-ones[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(6): 430-432,456. doi: 10.3969/j.issn.1006-0111.2012.06.009

Synthesis and biological activity of 1H-pyrrol-2(5H)-ones

doi: 10.3969/j.issn.1006-0111.2012.06.009
  • Received Date: 2012-05-11
  • Rev Recd Date: 2012-06-20
  • Objective To study the biological activity of 1H-pyrrol-2(5H)-ones which introduced substituted phenyl group as side chain. Methods By introduction of 5-substituted phenyl group, a serial 1H-pyrrol-2(5H)-ones were synthesized and their structures were confirmed by 1H NMR and MS. The binding constant Ki was assayed by the fluorescence polarization binding assay method. Results Thirteen title compounds exhibited stronger protein binding activities and compound 4e showed five times higher than positive drug. Conclusion The introduction of electron-attracting groups was beneficial to improve their activities. Among them, the nitro group was preferred group.
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Synthesis and biological activity of 1H-pyrrol-2(5H)-ones

doi: 10.3969/j.issn.1006-0111.2012.06.009

Abstract: Objective To study the biological activity of 1H-pyrrol-2(5H)-ones which introduced substituted phenyl group as side chain. Methods By introduction of 5-substituted phenyl group, a serial 1H-pyrrol-2(5H)-ones were synthesized and their structures were confirmed by 1H NMR and MS. The binding constant Ki was assayed by the fluorescence polarization binding assay method. Results Thirteen title compounds exhibited stronger protein binding activities and compound 4e showed five times higher than positive drug. Conclusion The introduction of electron-attracting groups was beneficial to improve their activities. Among them, the nitro group was preferred group.

ZHAO Fang-zhen, ZHUANG Chun-lin, GUO Zi-zhao, SHENG Chun-quan, YAO Jian-zhong, MIAO Zhen-yuan, ZHANG Wan-nian. Synthesis and biological activity of 1H-pyrrol-2(5H)-ones[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(6): 430-432,456. doi: 10.3969/j.issn.1006-0111.2012.06.009
Citation: ZHAO Fang-zhen, ZHUANG Chun-lin, GUO Zi-zhao, SHENG Chun-quan, YAO Jian-zhong, MIAO Zhen-yuan, ZHANG Wan-nian. Synthesis and biological activity of 1H-pyrrol-2(5H)-ones[J]. Journal of Pharmaceutical Practice and Service, 2012, 30(6): 430-432,456. doi: 10.3969/j.issn.1006-0111.2012.06.009
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