78832-95-8Relevant articles and documents
Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity
Jia, Ruifang,Zhang, Jian,Bertagnin, Chiara,Cherukupalli, Srinivasulu,Ai, Wei,Ding, Xiao,Li, Zhuo,Zhang, Jiwei,Ju, Han,Ma, Xiuli,Loregian, Arianna,Huang, Bing,Zhan, Peng,Liu, Xinyong
, (2021/01/05)
Encouraged by our earlier discovery of N1-selective inhibitors, the 150-cavity of influenza virus neuraminidases (NAs) could be further exploited to yield more potent oseltamivir derivatives. Herein, we report the design, synthesis and biological evaluation of a series of novel oseltamivir derivatives via the structural modifications at C5–NH2 of oseltamivir targeting 150-cavity. Among them, compound 5c bearing 4-(3-methoxybenzyloxy)benzyl group exhibited the most potent activity, which was lower or modestly improved activities than oseltamivir carboxylate (OSC) against N1 (H1N1), N1 (H5N1) and N1 (H5N1–H274Y). Specifically, there was 30-fold loss of activity against the wild-type strain H1N1. However, 5c displayed 4.85-fold more potent activity than OSC against H5N1–H274Y NA. Also, 5c demonstrated low cytotoxicity in vitro and no acute toxicity in mice. Molecular docking studies provided insights into the high potency of 5c against N1 and N1–H274Y mutant NAs. Besides, the in silico prediction of physicochemical properties and CYP enzymatic inhibitory ability of representative compounds were conducted to evaluate their drug-like properties.
Sulfonium salt containing pyrazoline groups and preparation method and application thereof
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Paragraph 0157-0158; 0163-0164, (2019/06/12)
The invention provides a sulfonium salt containing pyrazoline groups and a preparation method and an application thereof, wherein the general formula of the sulfonium salt is shown in the description;R and R are independently selected from hydroge
Novel diaryl sulfonium salt compound containing diphenylethene groups as well as preparation method and application thereof
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Paragraph 0097-0099; 0103; 0104; 0128-0130, (2018/09/13)
The invention relates to the technical field of new material organic chemicals, and particularly relates to a novel diaryl sulfonium salt shown as a formula (I) and having a diphenylethene conjugatedstructure, a chemical process preparation technique ther