N -monoarylacetothioureas as potent urease inhibitors: synthesis, SAR, and biological evaluation.
作者: Li Wei-YiNi Wei-WeiYe Ya-XiFang Hai-LianPan Xing-MingHe Jie-LingZhou Tian-LiYi JuanLiu Shan-ShanZhou MiXiao Zhu-PingZhu Hai-Liang
作者单位: 1National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse and Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, PR China.
2State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, PR China.
3National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for A
刊名: Journal of enzyme inhibition and medicinal chemistry, 2020, Vol.35 (1), pp.404-413
来源数据库: PubMed Journal
DOI: 10.1080/14756366.2019.1706503
关键词: Helicobacter pyloriN-monoarylacetothioureaSPRUrease inhibitorMolecular dynamics
原始语种摘要: A urease inhibitor with good in vivo profile is considered as an alternative agent for treating infections caused by urease-producing bacteria such as Helicobacter pylori . Here, we report a series of N -monosubstituted thioureas, which act as effective urease inhibitors with very low cytotoxicity. One compound ( b19 ) was evaluated in detail and shows promising features for further development as an agent to treat H. pylori caused diseases. Excellent values for the inhibition of b19 against both extracted urease and urease in intact cell were observed, which shows IC50 values of 0.16 ± 0.05 and 3.86 ± 0.10 µM, being 170- and 44-fold more potent than the clinically used drug AHA, respectively. Docking simulations suggested that the monosubstituted thiourea moiety penetrates...
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关键词翻译
关键词翻译
  • urease 尿素酶
  • thiourea 硫脲
  • moiety 一部分
  • potent 强大的
  • synthesis 合成
  • SAR Safe Address Register
  • Helicobacter 哈比特属
  • dissociation 解离
  • inhibitor 抑制剂
  • treating 处理