165682-82-6Relevant academic research and scientific papers
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.
Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4
Cheng, Xinlai,Yoshida, Hiroki,Raoofi, Dena,Saleh, Sawsan,Alborzinia, Hamed,Wenke, Frank,G?hring, Axel,Reuter, Stefanie,Mah, Nancy,Fuchs, Heiko,Andrade-Navarro, Miguel A.,Adjaye, James,Gul, Sheraz,Utikal, Jochen,Mrowka, Ralf,W?lfl, Stefan
, p. 5742 - 5750 (2015/08/24)
The octamer-binding transcription factor 4 (Oct3/4) is a master gene in the transcriptional regulatory network of pluripotent cells. Repression of Oct3/4 in embryonic stem cells (ESCs) is associated with cell differentiation and loss of pluripotency, wher
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
SUBSTITUTED THIAZOL-2-YLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS 11-BETA HSD1 MODULATORS
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Page/Page column 8-9, (2012/02/06)
The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11βHSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.
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.
5-CARBOXAMIDO SUBSTITUTED THIAZOLE DERIVATIVES THAT INTERACT WITH ION CHANNELS, IN PARTICULAR WITH ION CHANNELS FROM THE Kv FAMILY
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Page/Page column 58, (2010/11/08)
The present invention relates to compounds that interact with ion channels. In particular, the invention relates to compounds having the structural Formula having the structural Formula (I), (II), (III) or (IV), stereoisomers, tautomers, racemics, prodrugs, metabolites thereof, or a pharmaceutically acceptable salt and/or solvate thereof, wherein X, Y1, Y2, R1, n, R3, R8, R9, R10, L1, L2, Ar1 and Ar2 are defined in claim 1. The invention also relates to methods for preparing said compounds, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in methods for treatment of the human and animal body.
