Synthesis, structure-activity relationship and in vitro biological evaluation of N-arylethyl isoquinoline derivatives as Coxsackievirus B3 inhibitors |
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Authors: | Wang Yan-Xiang Li Yu-Huan Li Ying-Hong Gao Rong-Mei Wang Hui-Qiang Liu Yan-Xin Gao Li-Mei Lu Qiao-Ni Jiang Jian-Dong Song Dan-Qing |
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Affiliation: | Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. |
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Abstract: | Currently, there is no approved antiviral drug for the infection caused by enteroviruses. A series of novel N-arylethyl isoquinoline derivatives defined with substituents on the ring A and C were designed, synthesized and evaluated in vitro for their activities against Coxsackievirus B3 (CVB3). The primary structure-activity relationship revealed that substituents on the ring A were not beneficial for the activity. Among these analogs synthesized, compound 7f bearing a methylenedioxy at the R(4) and R(5) positions afforded an anti-CVB3 activity and a reasonable selectivity index (SI=26.8); furthermore, 7f exhibited a moderate activity against enterovirus 71 (EV71) with SI value of 9.0. Thus it has been selected as an anti-enteroviral lead compound for further investigation. |
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Keywords: | N-Arylethyl isoquinoline Coxsackievirus B3 Structure-activity relationship Enterovirus 71 Enteroviruses |
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