2. Academic Validation
  3. Novel 12N-substituted matrinanes as potential anti-coxsackievirus agents

Novel 12N-substituted matrinanes as potential anti-coxsackievirus agents

  • Bioorg Med Chem Lett. 2017 Feb 15;27(4):829-833. doi: 10.1016/j.bmcl.2017.01.022.
Ying-Hong Li 1,  Sheng Tang 1,  Yu-Huan Li 1,  Xin-Yue Cheng 1,  Xin Zhang 1,  Yan-Xiang Wang 1,  Feng Su 2,  Dan-Qing Song 3
Affiliations

Affiliations

  • 1 Institute of Medicinal Biotechnology, Chinese Academy of Medical Science & Peking Union Medical College, Beijing, China.
  • 2 College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, China. Electronic address: [email protected].
  • 3 Institute of Medicinal Biotechnology, Chinese Academy of Medical Science & Peking Union Medical College, Beijing, China. Electronic address: [email protected].
PMID: 28109785 DOI: 10.1016/j.bmcl.2017.01.022
Abstract

A series of novel 12N-substituted matrinane derivatives were synthesized and evaluated for their activities against coxsackievirus type B3 (CVB3) taking compound 1 as the lead. SAR analysis indicated that the introduction of a suitable heteroaromatic ring on the 12N-atom might be beneficial for the activity. Among them, compound 8a exhibited the highest potency against all CVB serotypes as well as CVA16 with IC50 values ranging from 2.02μM to 7.41μM, indicating a broad-spectrum anti-coxsackieviruse effect. Furthermore, compound 8a demonstrated a good safety profile in vivo. Thus, we consider 12N-substituted matrinanes to be a promising family of anti-coxsackievirus agents, and compound 8a to be a promising drug candidate in the treatment of various diseases related to coxsackievirus Infection.

Keywords

Broad-spectrum; Coxsakievirus; Druglike; Matrinane; Structure–activity relationship.

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