Synthesis and biological evaluation of 12-N-benzenesulfonyl matrinic ether derivatives as anti-coxsackievirus B3 agents
10.16438/j.0513-4870.2015-1011
- VernacularTitle:12-N-苯磺酰苦参醚衍生物的合成及其抗柯萨奇病毒B3活性研究
- Author:
Xin-yue CHENG
1
;
Sheng TANG
1
;
Lan-ying KONG
1
;
Yu-huan LI
1
;
Dan-qing SONG
1
Author Information
1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
matrinic ether;
sophocarpine;
coxsackievirus B3;
structure-activity relationship
- From:
Acta Pharmaceutica Sinica
2016;51(4):606-
- CountryChina
- Language:Chinese
-
Abstract:
12-N-m-Cyanobenzenesulfonyl matrinic butyl methyl ether is a potent anti-coxsackievirus B3(CVB3) agent bearing a novel structure skeleton. Taking this compound as a lead, totally 15 novel target compounds have been synthesized and evaluated for the anti-CVB3 activities using CPE method. Structureactivity relationship (SAR) demonstrated that the shorten-length of 11-side chain was not helpful for keeping the good anti-virus activity. Among the newly synthesized compounds, compound c1 displayed a good anti-CVB3 activity with the IC50 of 7.1 μmol·L-1 and SI of 35.5, similar to that of the lead. The SAR results provided useful information for further optimization of these compounds in the molecular structure.
