In:
Chemistry & Biodiversity, Wiley, Vol. 12, No. 4 ( 2015-04), p. 685-696
Abstract:
A series of novel isoflavonoids were synthesized based on structural modifications of daidzein, an active ingredient of traditional Chinese medicine (TCM) and evaluated for their anti‐influenza activity, in vitro , against H1N1 Tamiflu ‐resistant (H1N1 TR) virus in the MDCK cell line. Among them, 4‐oxo‐4 H ‐1‐benzopyran‐8‐carbaldehydes 11a – 11g were most promising, and they demonstrated better activities and selectivities comparable to those the reference ribarivin, a nucleoside antiviral agent. 3‐(4‐Bromophenyl)‐7‐hydroxy‐4‐oxo‐4 H ‐1‐benzopyran‐8‐carboxaldehyde ( 11c ) displayed the best inhibitory activity ( EC 50 , 29.0 μ M ) and selectivity index ( SI 〉 10.3). Analysis of the structureactivity relationships (SAR) indicated that both the non‐naturally‐occurring Br‐substituted B ‐ring and appropriate CHO and OH groups on the A ‐ring might be critical for the activity and selectivity against H1N1 TR influenza viruses.
Type of Medium:
Online Resource
ISSN:
1612-1872
,
1612-1880
DOI:
10.1002/cbdv.201400337
Language:
English
Publisher:
Wiley
Publication Date:
2015
detail.hit.zdb_id:
2139001-0
SSG:
12
