566205-01-4Relevant articles and documents
Synthesis, Structure-Activity Relationships, and Antiviral Activity of Allosteric Inhibitors of Flavivirus NS2B-NS3 Protease
Nie, Shenyou,Yao, Yuan,Wu, Fangrui,Wu, Xiaowei,Zhao, Jidong,Hua, Yuanda,Wu, Jingyu,Huo, Tong,Lin, Yi-Lun,Kneubehl, Alexander R.,Vogt, Megan B.,Ferreon, Josephine,Rico-Hesse, Rebecca,Song, Yongcheng
, p. 2777 - 2800 (2021)
Flaviviruses, including Zika, dengue, and West Nile viruses, are important human pathogens. The highly conserved NS2B-NS3 protease of Flavivirus is essential for viral replication and therefore a promising drug target. Through compound screening, followed by medicinal chemistry studies, a novel series of 2,5,6-trisubstituted pyrazine compounds are found to be potent, allosteric inhibitors of Zika virus protease (ZVpro) with IC50 values as low as 130 nM. Their structure-activity relationships are discussed. The ZVpro inhibitors also inhibit homologous proteases of dengue and West Nile viruses, and their inhibitory activities are correlated. The most potent compounds 47 and 103 potently inhibited Zika virus replication in cells with EC68 values of 300-600 nM and in a mouse model of Zika infection. These compounds represent novel pharmacological leads for drug development against Flavivirus infections.
Concise Synthesis of v-Coelenterazines
Hosoya, Takamitsu,Iimori, Rie,Yoshida, Suguru,Sumida, Yuto,Sahara-Miura, Yuiko,Sato, Jun-Ichi,Inouye, Satoshi
supporting information, p. 3888 - 3891 (2015/08/18)
A novel synthetic method for v-coelenterazine (v-CTZ), which is a vinylene-bridged analog of native CTZ with a large red-shifted luminescence property, is described. The synthesis was achieved in a concise way through the use of three sequential cross-cou
PYRROLO[2,3-B]PYRAZINES AS SYK INHIBITORS
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Page/Page column 88, (2014/03/25)
The present invention relates to the use of novel pyrrolo[2,3- b]]pyrazines wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.