Chinese Journal of Organic Chemistry >
Synthesis and Evaluation of the Antischistosomal Activity against S. japonicum of 1-Methyl-1,2,3,4-tetrahydroisoquinoline Derivatives
Received date: 2013-08-14
Revised date: 2013-09-28
Online 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.
Wang Wenlong , Song Lijun , Wang Guping , Fan Wenhua , Yin Xuren , Yu Chuanxin , Feng Bainian . Synthesis and Evaluation of the Antischistosomal Activity against S. japonicum of 1-Methyl-1,2,3,4-tetrahydroisoquinoline Derivatives[J]. Chinese Journal of Organic Chemistry, 2013 , 33(12) : 2588 -2595 . DOI: 10.6023/cjoc201308017
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