165682-82-6Relevant articles and documents
Disrupting the Conserved Salt Bridge in the Trimerization of Influenza A Nucleoprotein
Woodring, Jennifer L.,Lu, Shao-Hung,Krasnova, Larissa,Wang, Shih-Chi,Chen, Jhih-Bin,Chou, Chiu-Chun,Huang, Yi-Chou,Cheng, Ting-Jen Rachel,Wu, Ying-Ta,Chen, Yu-Hou,Fang, Jim-Min,Tsai, Ming-Daw,Wong, Chi-Huey
, p. 205 - 215 (2020/01/02)
Antiviral drug resistance in influenza infections has been a major threat to public health. To develop a broad-spectrum inhibitor of influenza to combat the problem of drug resistance, we previously identified the highly conserved E339?R416 salt bridge of the nucleoprotein trimer as a target and compound 1 as an inhibitor disrupting the salt bridge with an EC50 = 2.7 μM against influenza A (A/WSN/1933). We have further modified this compound via a structure-based approach and performed antiviral activity screening to identify compounds 29 and 30 with EC50 values of 110 and 120 nM, respectively, and without measurable host cell cytotoxicity. Compared to the clinically used neuraminidase inhibitors, these two compounds showed better activity profiles against drug-resistant influenza A strains, as well as influenza B, and improved survival of influenza-infected mice.
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore
Washburn, David G.,Holt, Dennis A.,Dodson, Jason,McAtee, Jeff J.,Terrell, Lamont R.,Barton, Linda,Manns, Sharada,Waszkiewicz, Anna,Pritchard, Christina,Gillie, Dan J.,Morrow, Dwight M.,Davenport, Elizabeth A.,Lozinskaya, Irina M.,Guss, Jeffrey,Basilla, Jonathan B.,Negron, Lorena Kallal,Klein, Michael,Willette, Robert N.,Fries, Rusty E.,Jensen, Timothy C.,Xu, Xiaoping,Schnackenberg, Christine G.,Marino Jr., Joseph P.
supporting information, p. 4979 - 4984 (2013/09/02)
Lead optimization of piperidine amide HTS hits, based on an anilino-thiazole core, led to the identification of analogs which displayed low nanomolar blocking activity at the canonical transient receptor channels 3 and 6 (TRPC3 & 6) based on FLIPR (carbac
THIAZOLES DERIVATIVES AS AMPK ACTIVATOR
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Page/Page column 36, (2008/06/13)
The present application provides novel thiazole derivatives that are useful as activators of Adenosine 5'-Monophosphate-Activated Protein Kinase and pharmaceutical compositions containing such compounds.