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Yong, Jian-Ping,Aisa, Haji Akber Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.4
To improve the biological activities of rupestonic acid, 21 new rupestonic acid fatty ester derivatives (2a-2h) and aromatic ester derivatives (2i-2u) were synthesized and preliminarily evaluated for their anti-influenza activity in vitro by the national center for drug screening of China, using the Oseltamivir and Ribavirin as reference drugs. The results showed that 2l ($IC_{50}=0.5{\mu}mol/L$) exhibited potent anti-influenza $A_3$ viral activity among the synthesized compounds and was 10-fold more potent than that of the reference drug Oseltamivir ($IC_{50}=5.1{\mu}mol/L$).
Jian-ping Yong,Haji Akber Aisa 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.4
To improve the biological activities of rupestonic acid, 21 new rupestonic acid fatty ester derivatives (2a-2h)and aromatic ester derivatives (2i-2u) were synthesized and preliminarily evaluated for their anti-influenza activity in vitro by the national center for drug screening of China, using the Oseltamivir and Ribavirin as reference drugs. The results showed that 2l (IC_50 = 0.5 μmol/L) exhibited potent anti-influenza A_3 viral activity among the synthesized compounds and was 10-fold more potent than that of the reference drug Oseltamivir (IC_50 = 5.1 μmol/L).
Yong, Jian-Ping,Lv, Qiao-Ying,Aisa, Haji Akber Korean Chemical Society 2009 Bulletin of the Korean Chemical Society Vol.30 No.2
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 $A_3$,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 $A_3\;(TC_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;19.2\;{\mu}$mol/L, SI = 6.3) and B (T$C_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;29.9\;{\mu}$mol/L, SI = 4.0); 2g was more active against influenza $A_3$ virus at very low cytotoxicity ($TC_{50}\;>\;2092.1\;{\mu}mol/L,\;IC_{50}=\;143.7\;{\mu}mol/L,$ 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 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;11.3\;{\mu}mol$/L, SI = 17.7 ) and HSV-2 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;20.7\;{\mu}mol$/L , SI = 9.7).
Jian-ping Yong,Qiao-ying Lv,Haji Akber Aisa 대한화학회 2009 Bulletin of the Korean Chemical Society Vol.30 No.2
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).