Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (12): 2588-2595.DOI: 10.6023/cjoc201308017 Previous Articles     Next Articles



王文龙a,b, 宋丽君c, 王古平a, 范文华b, 殷旭仁c, 余传信c, 冯柏年a,b   

  1. a 江南大学药学院 无锡 214122;
    b 江苏艾凡生物医药有限公司 无锡 214122;
    c 江苏省寄生虫病防治研究所 无锡 214064
  • 收稿日期:2013-08-14 修回日期:2013-09-28 发布日期:2013-10-10
  • 通讯作者: 冯柏年, 余传信;
  • 基金资助:

    国家自然科学基金(No. 30972581)、江苏省自然科学基金(No. BK2008110)、江苏省兴卫工程平台(No. ZX201108)和中央高校基本科研业务费(No. JUSRP1040)资助项目.

Synthesis and Evaluation of the Antischistosomal Activity against S. japonicum of 1-Methyl-1,2,3,4-tetrahydroisoquinoline Derivatives

Wang Wenlonga,b, Song Lijunc, Wang Gupinga, Fan Wenhuab, Yin Xurenc, Yu Chuanxinc, Feng Bainiana,b   

  1. a School of Pharmaceutical Science, Jiangnan University, Wuxi 214122;
    b Jiangshu Alpha Biopharmaceuticals, Inc., Wuxi 214122;
    c Jiangsu Institute of Parasitic Diseases, Wuxi 214064
  • Received:2013-08-14 Revised:2013-09-28 Published:2013-10-10
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 30972581), the Natural Science Foundation of Jiangsu Province (No. BK2008110), the Health Promotion Project Foundation of Jiangsu Province (No. ZX201108), and the Fundamental Research Funds for the Central Universities (No. JUSRP1040).

Due to widespread and intensive use of antischistosomal drug, praziquantel (PZQ), there is serious concern that drug-resistant mutants of the parasite may emerge. To develop novel antischistosomal agents, a series of 1-methyl-1,2,3,4-tetrahydroisoquinoline derivatives were designed, synthesized, and evaluated for their antischistosomal activity against S. japonicum in vitro. The results indicated that compound 10 with chloroacetyl group showed better antischistosoaml activity than PZQ.

Key words: praziquantel, 1-methyl-1,2,3,4-tetrahydroisoquinoline derivatives, Schistosoma japonicum, antischistosomal activity