Design and Synthesis of Benzoyl Andrographolde Derivatives as Potential Dual-function Agents for Anti-influenza Therapy

Chia Nan University of Pharmacy & Science Institutional Repository > 藥理學院 > 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會 > Item 310902800/24244

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標題:	Design and Synthesis of Benzoyl Andrographolde Derivatives as Potential Dual-function Agents for Anti-influenza Therapy
作者:	Chin-Yi Ko (柯勤益) Wen-Hsin Huang (黃文鑫) An-Rong Lee (李安榮)
日期:	2011
上傳時間:	2011-06-23 14:57:31 (UTC+8)
摘要:	The World Health Organization (WHO) recommended the use of neuraminidase inhibitors (NAIs) oseltamivir and zanamivir, as the guideline for anti-influenza therapy. However, more than 2UU cases 01 oseltamivir-resistant virus infection have been reported worldwide. The mechanism of drug resistance due to the rapid evolution *n of virus and the functional balance between neuraminidase and haemagglutinin, therefore, the development of multi-mechanism-based drugs is an effective strategy to combat the resistant strain-infection. According to 'airplane model', I used two benzoic acid derivatives, 1 and 9, as starting materials for synthesizing novel aromatic NAIs. Besides, andrographolide, the active component of A. paniculata was reported that it has potent haemagglutinin inhibitory activity. Furthermore, the goal of incorporation of benzoic acid derivatives and andrographolide is in progress to synthesize a series of anti-influenza agents. The ability of the synthetic compounds to interfere with the plaque formation by human influenza viruses was examined on the basis of the maximum non-toxic concentration of the test compounds. Some of our products showed potent activity, in vitro, against anti-HlNl viruses. Further investigations on the mechanisms of action are in progress.
關聯:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
顯示於類別:	[藥理學院] 2011年台俄有機、藥物與生物化學交流暨藥物化學研討會

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