Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives.
10.1016/j.apsb.2014.06.003
- Author:
Situ XUE
1
;
Linlin MA
1
;
Rongmei GAO
1
;
Yuhuan LI
1
;
Zhuorong LI
1
Author Information
1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- Keywords:
Broad-spectrum antiviral activity;
DNA and RNA virus;
Indole-2-carboxylate;
SAR
- From:
Acta Pharmaceutica Sinica B
2014;4(4):313-321
- CountryChina
- Language:English
-
Abstract:
A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compound 8f showed the highest SI value (17.1) to Cox B3 virus. Compound 14f showed both potent inhibitory activity against influenza A (IC50=7.53 μmol/L) and the highest SI value (12.1). SAR results showed that the alkyloxy at the 4-position of indole ring was not crucial to the antiviral activities. Incorporation of an acetyl substituent at the amino group disfavored antiviral activity towards RNA viruses.
