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Decoquinate derivatives: A new class of potent antischistosomal agents against Schistosoma japonicum
  • ISSN号:1001-8417
  • 期刊名称:《中国化学快报:英文版》
  • 时间:0
  • 分类:S852.735[农业科学—基础兽医学;农业科学—兽医学;农业科学—畜牧兽医] O626.323[理学—有机化学;理学—化学]
  • 作者机构:[1]School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China, [2]Key Laboratory of National Health and Family Planning Commission on Parasitic Disease Control and Prevention, Jiangsu Provincial Key Laboratory on Parasite and Vector Control Technology, Jiangsu Institute of Parasitic Diseases, Wuxi 214064, China, [3]Medical School, Jiangnan University, Wuxi 214122, China, [4]Suzhou Kemu Veterinary Pharmaceutical Co., Ltd., Meiyan High-technology Development Zone, Suzhou 215225, China
  • 相关基金:Acknowledgements This work was supported by Laboratory Research Fund funded by Key Laboratory of National Health and Family Planning Commission on Parasitic Disease Control and Prevention, Jiangsu Provincial Key Laboratory on Parasite and Vector Control Technology, Parasitic Disease Prevention and Control Platform (No. WK014-002), fund from the Department of Science and Technology of Jiangsu Province (No. BY2016022-37), fund from the National Natural Science Foundation of China (Nos. 21472069, 30972581, 8120316), fund from the Natural Science Foundation of Jiangsu Province (Nos. BK2012544, BK20151120), fund from the scientific research projects of Jiangsu Provincial Commission of Health and Family Planning (No. H201635), fund from the scientific research projects of Wuxi City Commission of Health and Family Planning (No. Q201656), fund from the Ministry of Education of China (No. JUSRP51516) and Jiangsu Science and Technology Department (No. BM2015024).
中文摘要:

Decoquinate (1 ) ,旧、便宜的 coccidiostat,展出有势力抗疟药活动然而,它对血吸虫 japonicum 的 antischistosomal 活动还没被评估了。基于 decoquinate,一系列 decoquinate 衍生物被设计,综合,与 S 作为 antischistosomal 代理人的一个新班作比较。在 vitro 的 japonicum 成年人蠕虫。在他们之中,混合 15 杀死的 100% 成年 S。在 72 的 japonicum ? 在 10 的集中的 h ? 在 vitro 的 mol/L,在 vitro 比 PZQ 展出了更强壮的杀死蠕虫的活动并且能用作有希望的铅混合物开发新 antischistosomal 代理人。

英文摘要:

Decoquinate(1), an old and inexpensive coccidiostat, exhibited potent antimalarial activity, however, its antischistosomal activity against Schistosoma japonicum has not yet been evaluated. Based on decoquinate, a series of decoquinate derivatives was designed, synthesized, evaluated as a new class of antischistosomal agents against S. japonicum adult worms in vitro. Among them, compound 15 killed 100% of adult S. japonicum in 72 h at the concentration of 10 mmol/L in vitro, exhibited stronger wormkilling activity than PZQ in vitro and could serve as a promising lead compound to develop new antischistosomal agents.

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期刊信息
  • 《中国化学快报:英文版》
  • 中国科技核心期刊
  • 主管单位:中国科学技术协会
  • 主办单位:中国化学会
  • 主编:
  • 地址:北京市先农坛街1号
  • 邮编:100050
  • 邮箱:cclbj@imm.ac.cn
  • 电话:010-63165638
  • 国际标准刊号:ISSN:1001-8417
  • 国内统一刊号:ISSN:11-2710/O6
  • 邮发代号:2-915
  • 获奖情况:
  • 1998、1999年获中国科协和国家自然科学基金,高科技学术期刊资助二等奖,2000年获国家自然基金委重点期刊一等奖
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  • 被引量:760