2. Academic Validation
  3. Synthesis, structure-activity relationship and in vitro biological evaluation of N-arylethyl isoquinoline derivatives as Coxsackievirus B3 inhibitors

Synthesis, structure-activity relationship and in vitro biological evaluation of N-arylethyl isoquinoline derivatives as Coxsackievirus B3 inhibitors

  • Bioorg Med Chem Lett. 2011 Oct 1;21(19):5787-90. doi: 10.1016/j.bmcl.2011.08.002.
Yan-Xiang Wang 1,  Yu-Huan Li,  Ying-Hong Li,  Rong-Mei Gao,  Hui-Qiang Wang,  Yan-Xin Liu,  Li-Mei Gao,  Qiao-Ni Lu,  Jian-Dong Jiang,  Dan-Qing Song
Affiliations

Affiliation

  • 1 Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
PMID: 21880491 DOI: 10.1016/j.bmcl.2011.08.002
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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