163461-00-5Relevant articles and documents
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses
Zhao, Xin,Li, Runfeng,Zhou, Yang,Xiao, Mengjie,Ma, Chunlong,Yang, Zhongjin,Zeng, Shaogao,Du, Qiuling,Yang, Chunguang,Jiang, Haiming,Hu, Yanmei,Wang, Kefeng,Mok, Chris Ka Pun,Sun, Ping,Dong, Jianghong,Cui, Wei,Wang, Jun,Tu, Yaoquan,Yang, Zifeng,Hu, Wenhui
, p. 5187 - 5198 (2018/06/04)
Influenza pandemic is a constant major threat to public health caused by influenza A viruses (IAVs). IAVs are subcategorized by the surface proteins hemagglutinin (HA) and neuraminidase (NA), in which they are both essential targets for drug discovery. While it is of great concern that NA inhibitor oseltamivir resistant strains are frequently identified from human or avian influenza virus, structural and functional characterization of influenza HA has raised hopes for new antiviral therapies. In this study, we explored a structure-activity relationship (SAR) of pinanamine-based antivirals and discovered a potent inhibitor M090 against amantadine-resistant viruses, including the 2009 H1N1 pandemic strains, and oseltamivir-resistant viruses. Mechanism of action studies, particularly hemolysis inhibition, indicated that M090 targets influenza HA and it occupied a highly conserved pocket of the HA2 domain and inhibited virus-mediated membrane fusion by locking the bending state of HA2 during the conformational rearrangement process. This work provides new binding sites within the HA protein and indicates that this pocket may be a promising target for broad-spectrum anti-influenza A drug design and development.
FORMYLTHIOPHENES AND THEIR USE IN FLAVOR AND FRAGRANCE COMPOSITIONS
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Page/Page column 19; 20, (2017/05/19)
The present invention is directed to novel organoleptic compounds, a process of augmenting, enhancing or imparting taste to a material selected from the group consisting of a foodstuff, a chewing gum, a dental product, an oral hygiene product and a medicinal product comprising the step of incorporating an olfactory acceptable amount of such novel organoleptic compounds, and a process of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of such novel organoleptic compounds.