171846-13-2Relevant academic research and scientific papers
Nanoparticular Inhibitors of Flavivirus Proteases from Zika, West Nile and Dengue Virus Are Cell-Permeable Antivirals
Arkona, Christoph,Bartenschlager, Ralf,Bergemann, Silke,Demirel, Peter,Fischer, Christina,Kallis, Stephanie,Masri, Enaam,Nitsche, Christoph,Rademann, J?rg,Redl, Lisa,Rudolf, Thomas,Schroeder, Barbara
supporting information, p. 1955 - 1961 (2021/12/09)
Viral proteases have been established as drug targets in several viral diseases including human immunodeficiency virus and hepatitis C virus infections due to the essential role of these enzymes in virus replication. In contrast, no antiviral therapy is a
Structure-activity studies of cyclic ketone inhibitors of the serine protease plasmin: Design, synthesis, and biological activity
Xue, Fengtian,Seto, Christopher T.
, p. 8467 - 8487 (2008/02/05)
Three series of cyclic ketone inhibitors were synthesized and evaluated against the serine protease plasmin. Peptide inhibitors that incorporated 3-oxotetrahydrofuran and 3-oxotetrahydrothiophene 1,1-dioxide groups had the highest activities. Alkylamino substituents, which were designed to bind in the S1 subsite of plasmin, were attached to the inhibitors. Compounds 5c and 5g, which incorporated 6-aminohexyl substituents, were found to be optimal and demonstrated IC50 values in the low micromolar range. Incorporating conformationally constrained peptide segments into the inhibitors did not improve their activities.
Pyrimidine derivatives useful as inhibitors of PKC-theta
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Page/Page column 137, (2008/06/13)
Disclosed are novel compounds of formula (I): wherein X, Y, R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective αVβ3 antagonists
Kling, Andreas,Backfisch, Gisela,Delzer, Juergen,Geneste, Herve,Graef, Claudia,Holzenkamp, Uta,Hornberger, Wilfried,Lange, Udo E.W,Lauterbach, Arnulf,Mack, Helmut,Seitz, Werner,Subkowski, Thomas
, p. 441 - 446 (2007/10/03)
Synthesis and SARs of new integrin αVβ3 antagonists based on an N-substituted dibenzazepinone scaffold are described. Variation of spacer and guanidine mimetic led to potent compounds exhibiting an IC50 towards αVβ3 in the nanomolar range, high selectivity versus integrin αIIbβ3 and efficacy in functional cellular assays.
