title: Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors.
abstract: The influenza virus is a persistent cause of mortality and morbidity on an annual basis and thus presents itself as an important target for pharmaceutical investigation. In this work, substituted bisaryl amide compounds were found to be a new class of potential anti-influenza agents, and a series of substituted bisaryl amide compounds were synthesised and evaluated for their anti-influenza virus activities. The analysis of the results produced a preliminary structure-activity relationship study (SAR). Compounds 1a, 1g, 1h, 1j, 1l and 1n exhibited clear antiviral activities against the influenza A (A/Guangdong Luohu/219/2006, H1N1) virus with 50% inhibitory concentrations (IC(50)) for virus growth ranging from 12.5 to 59.0 μM. Specifically, compound 1j also possessed antiviral activity against both oseltamivir-resistant influenza (A/Jinnan/15/2009) virus and influenza B (B/Jifang/13/97) virus with IC(50) values of 9.2 μM and 21.4 μM, respectively. Compound 1j is thus worth further investigation as an anti-influenza virus candidate.
authors: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
authors: Lan-hu
authors: LH
authors: Hao
authors: Yan-ping
authors: YP
authors: Li
authors: Wei-ying
authors: WY
authors: He
authors: Hui-qiang
authors: HQ
authors: Wang
authors: Guang-zhi
authors: GZ
authors: Shan
authors: Jian-dong
authors: JD
authors: Jiang
authors: Yu-huan
authors: YH
authors: Li
authors: Zhuo-rong
authors: ZR
authors: Li
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects*; D009981:Influenza B virus / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000998:Antiviral Agents