4.7 Article

Decoquinate derivatives: A new class of potent antischistosomal agents against Schistosoma japonicum

Journal

CHINESE CHEMICAL LETTERS
Volume 28, Issue 7, Pages 1547-1552

Publisher

ELSEVIER SCIENCE INC
DOI: 10.1016/j.cclet.2017.03.036

Keywords

Decoquinate Derivatives; Worm-killing activity; Schistosoma japonicum; Structure activity relationships (SARs)

Funding

  1. Laboratory Research Fund - Key Laboratory of National Health and Family Planning Commission on Parasitic Disease Control and Prevention
  2. Jiangsu Provincial Key Laboratory on Parasite and Vector Control Technology
  3. Parasitic Disease Prevention and Control Platform [WK014-002]
  4. Department of Science and Technology of Jiangsu Province [BY2016022-37]
  5. National Natural Science Foundation of China [21472069, 30972581, 8120316]
  6. Natural Science Foundation of Jiangsu Province [BK2012544, BK20151120]
  7. scientific research projects of Jiangsu Provincial Commission of Health and Family Planning [H201635]
  8. scientific research projects of Wuxi City Commission of Health and Family Planning [Q201656]
  9. Ministry of Education of China [JUSRP51516]
  10. Jiangsu Science and Technology Department [BM2015024]

Ask authors/readers for more resources

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 mu mol/L. in vitro, exhibited stronger worm killing activity than PZQ in vitro and could serve as a promising lead compound to develop new antischistosomal agents. (C) 2017 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.

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