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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 30, Number 2
BKCSDE 30(2)
February 20, 2009 

Synthesis of (5R,8R)-2-(3,8-Dimethyl-2-oxo-1,2,4,5,6,7,8,8α-octahydroazulen-5-yl)
Acrylic Acid (Rupestonic Acid) Amide Derivatives and in vitro Inhibitive Activities
against Influenza A3,B and Herpes Simplex Type 1 and 2 Virus
Jian ping Yong, Qiao ying Lv, Haji Akber Aisa*
Synthesis, Rupestonic acid amide derivative, Anti-viral activities
19 Aromatic ring and L-amino acid ester contained rupestonic acid amide derivatives 2a~2l, 3a~3g were synthesized and preliminarily evaluated in vitro against influenza virus A3,B and herpes simplex virus type 1 (HSV-1), 2(HSV-2) by the national center for drug screening of China. The rusults showed that 2i possessed the highest inhibition against both influenza virus A3 (TC50 = 120.6 μmol/L, IC50 = 19.2 μmol/L, SI = 6.3) and B (TC50 = 120.6 μmol/L, IC50 = 29.9 μmol/L, SI = 4.0); 2g was more active against influenza A3 virus at very low cytotoxicity (TC50 > 2092.1 μmol/L, IC50 = 143.7 μmol/L, SI > 14.6) than the parent compound; Compounds 2b, 2c, 2f showed higher activities both against HSV-1 and HSV-2 than that of the parent compound, and 2f was the most potent inhibitor of HSV-1 (TC50 = 200.0 μmol/L, IC50 = 11.3 μmol/L, SI = 17.7 ) and HSV-2 (TC50 = 200.0 μmol/L, IC50 = 20.7 μmol/L , SI = 9.7).
435 - 440
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