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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
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  • 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
  • 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
저자명
Yong. Jian-Ping,Lv. Qiao-Ying,Aisa. Haji Akber
간행물명
Bulletin of the Korean Chemical Society
권/호정보
2009년|30권 2호|pp.435-440 (6 pages)
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대한화학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

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).