76274-94-7Relevant academic research and scientific papers
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation
Pulz, Robert,Angst, Daniela,Dawson, Janet,Gessier, Francois,Gutmann, Sascha,Hersperger, Rene,Hinniger, Alexandra,Janser, Philipp,Koch, Guido,Revesz, Laszlo,Vulpetti, Anna,Waelchli, Rudolf,Zimmerlin, Alfred,Cenni, Bruno
supporting information, p. 1467 - 1472 (2019/10/11)
Bruton's tyrosine kinase (BTK) is a member of the TEC kinase family and is selectively expressed in a subset of immune cells. It is a key regulator of antigen receptor signaling in B cells and of Fc receptor signaling in mast cells and macrophages. A BTK
Chemical and biological investigation of cyclopropyl containing diaryl-pyrazole-3-carboxamides as novel and potent cannabinoid type 1 receptor antagonists
Szabó, Gyorgy,Varga, Balázs,Páyer-Lengyel, Dóra,Szemzo, Attila,Erdélyi, Péter,Vukics, Krisztina,Szikra, Judit,Hegyi, éva,Vastag, Mónika,Kiss, Béla,Laszy, Judit,Gyertyán, István,Fischer, János
experimental part, p. 4329 - 4337 (2010/02/28)
Obesity is a major clinical problem in the western world, and many molecular targets have been explored in the search for effective therapeutic agents. One of these, antagonism of the cannabinoid 1 (CB1) receptor, rose to prominence following reports demo
MYOSIN LIGHT CHAIN PHOSPHATASE INHIBITORS
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Page/Page column 61-62, (2009/12/27)
Novel myosin light chain phosphatase inhibitors, compositions containing them, methods of making and using them, and methods of using fluorescent myosin light chain phosphatase inhibitors are described.
Synthesis and Antiinflammatory and Analgesic Activity of 5-Aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolopyrrole-1-carboxylic Acids and 1-Methyl-4-(methylthio)-5-aroylpyrrole-2-acetic Acids
Muchowski, Joseph M.,Galeazzi, Edvige,Greenhouse, Robert,Guzman, Angel,Perez, Virginia,et al.
, p. 1202 - 1207 (2007/10/02)
5-Aroyl-6-(methylthio)-1,2-dihydro-3H-pyrrolopyrrole-1-carboxylic acids and 1-methyl-4-(methylthio)-5-aroylpyrrole-2-acetic acids were synthesized and assayed as antiinflammatory and analgesic agents.The majority of these compounds exhibit a surpri
Carbon-13 Nuclear Maagnetic Resonance Spectroscopy. Substituent-induced Chemical Shift Effects on Cyclopropyl Carbons of 4-Substituted Cyclopropylbenzenes
Kusuyama, Yoshiaki,Dyllick-Brenzinger, Christina,Roberts, John D.
, p. 372 - 375 (2007/10/02)
Carbon-13 chemical shifts of the cyclopropyl carbons of eleven 4-substituted cyclopropylbenzenes have been measured under conditions effectively corresponding to infinite dilution in DCCl3.The substituent-induced chemical shifts (SCS) of both the α and β carbons of the cyclopropane ring were found to be downfield with electron-attracting groups and upfield for electron-donating groups.The trends for the β carbons correspond to those observed for the β carbons of 4-substituted phenylethenes, while the trends of the α carbons are similar to those found for the α carbons of 4-substituted isopropyl benzenes.The results for the β carbons can be rationalized by postulating a substantial contribution from a hyperconjugative resonance effect involving the ? system of the benzene ring (and its 4-substituent) and C-α--C-β bonds of the cyclopropane ring.The effects on the α carbons are in accord with a very resonable smaller inductive polarization of the C-α--C-β bonds than encountered for the carbons of corresponding ethenyl- or ethynylbenzenes.
