Dang Zhao, Jung Katherine, Zhu Lei, Xie Hua, Lee Kuo-Hsiung, Chen Chin-Ho, Huang Li
Surgical Science, Department of Surgery, Duke University Medical Center , Durham, North Carolina 27710, United States.
School of Dentistry, Meharry Medical College , Nashville, Tennessee 37208, United States.
ACS Med Chem Lett. 2015 Jan 29;6(3):355-8. doi: 10.1021/ml500533x. eCollection 2015 Mar 12.
A series of diterpenoid derivatives based on podocarpic acid were synthesized and evaluated as anti-influenza A virus agents. Several of the novel podocarpic acid derivatives exhibited nanomolar activities against an H1N1 influenza A virus (A/Puerto Rico/8/34) that was resistant to two anti-influenza drugs, oseltamivir and amantadine. This class of compounds inhibits the influenza virus by targeting the viral hemagglutinin-mediated membrane fusion. These results indicated that podocarpic acid derivatives may serve as potential drug candidates to fight drug-resistant influenza A virus infections.
合成了一系列基于罗汉松酸的二萜类衍生物，并将其作为抗甲型流感病毒药物进行评估。几种新型罗汉松酸衍生物对一种对两种抗流感药物（奥司他韦和金刚烷胺）耐药的H1N1甲型流感病毒（A/波多黎各/8/34）表现出纳摩尔活性。这类化合物通过靶向病毒血凝素介导的膜融合来抑制流感病毒。这些结果表明，罗汉松酸衍生物可能作为对抗耐药甲型流感病毒感染的潜在候选药物。
