20324-49-6Relevant academic research and scientific papers
Discovery of Ziresovir as a Potent, Selective, and Orally Bioavailable Respiratory Syncytial Virus Fusion Protein Inhibitor
Zheng, Xiufang,Gao, Lu,Wang, Lisha,Liang, Chungen,Wang, Baoxia,Liu, Yongfu,Feng, Song,Zhang, Bo,Zhou, Mingwei,Yu, Xin,Xiang, Kunlun,Chen, Li,Guo, Tao,Shen, Hong C.,Zou, Gang,Wu, Jim Zhen,Yun, Hongying
supporting information, p. 6315 - 6329 (2019/07/09)
Ziresovir (RO-0529, AK0529) is reported here for the first time as a promising respiratory syncytial virus (RSV) fusion (F) protein inhibitor that currently is in phase 2 clinical trials. This article describes the process of RO-0529 as a potent, selective, and orally bioavailable RSV F protein inhibitor and highlights the in vitro and in vivo anti-RSV activities and pharmacokinetics in animal species. RO-0529 demonstrates single-digit nM EC50 potency against laboratory strains, as well as clinical isolates of RSV in cellular assays, and more than one log viral load reduction in BALB/c mouse model of RSV viral infection. RO-0529 was proven to be a specific RSV F protein inhibitor by identification of drug resistant mutations of D486N, D489V, and D489Y in RSV F protein and the inhibition of RSV F protein-induced cell-cell fusion in cellular assays.
1,3-BENZOTHIAZINONE DERIVATIVE AND USE THEREOF
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Page/Page column 20, (2008/06/13)
The present invention provides compounds represented by formula (I): wherein R1 independently represents a halogen atom, hydroxy, nitro, an optionally halogenated alkyl, alkenyl or alkynyl, an optionally substituted alkoxy, an acyl, or an optionally substituted amino; R2 represents hydrogen atom or an optionally substituted hydrocarbon group; R3 represents an electron-withdrawing group; n represents an integer of 0 to 2; and m represents an integer of 1 to 6 (hereinafter sometimes briefly referred to as Compound (I)); or salts thereof. These compounds are capable of binding to macrophage migration inhibitory factor (MIF) and useful as agents for preventing/treating diseases induced by oxidative stress.
Novel inhibitors of the prenylated protein methyltransferase reveal distinctive structural requirements
Marciano, Daniele,Aharonson, Ziporet,Varsano, Tal,Haklai, Roni,Kloog, Yoel
, p. 1709 - 1714 (2007/10/03)
Inhibitors of a prenylated protein methyltransferase were synthesized and evaluated. S-farnesyl-5-fluorothiosalicylic acid and the 5-chloro analog (but not the 4-fluoro, 4-chloro or 3-chloro analogs) were potent inhibitors, as was the parent compound S-farnesyl thiosalicylic acid (FTS), whose methyl ester was far less active. S-geranyl and S-geranylgeranyl thiosalicylic acids were more than ten times less potent than FTS.
