- Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis
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In recent years, channels that mediate store-operated calcium entry (SOCE, i.e., the ability of cells to sense a decrease in endoplasmic reticulum luminal calcium and induce calcium entry across the plasma membrane) have been associated with a number of d
- Riva, Beatrice,Griglio, Alessia,Serafini, Marta,Cordero-Sanchez, Celia,Aprile, Silvio,Di Paola, Rosanna,Gugliandolo, Enrico,Alansary, Dalia,Biocotino, Isabella,Lim, Dmitry,Grosa, Giorgio,Galli, Ubaldina,Niemeyer, Barbara,Sorba, Giovanni,Canonico, Pier Luigi,Cuzzocrea, Salvatore,Genazzani, Armando A.,Pirali, Tracey
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p. 9756 - 9783
(2018/11/23)
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- MODULATORS OF SOCE, COMPOSITIONS, AND USES THEREOF
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Compounds of Formula (I) able to modulate Store Operated Calcium Entry (SOCE). The disclosure also relates to the use of compounds of formula (I) for treatment of pathological conditions in which SOCE modulation might be beneficial, such as neglecting dis
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- Microwave-assisted and continuous flow multistep synthesis of 4-(pyrazol-1-yl)carboxanilides
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A series of 4-(pyrazol-1-yl)carboxanilides active as inhibitors of canonical transient receptor potential channels were synthesized in an efficient three-step protocol using controlled microwave heating. The general synthetic strategy involves condensation of 4-nitrophenylhydrazine with appropriate 1,3-dicarbonyl building blocks, followed by reduction of the nitro group to the amine, which is then amidated with carboxylic acids. Compared to the conventional protocol a dramatic reduction in overall processing time from ～2 days to a few minutes was achieved, accompanied by significantly improved product yields. In addition, the first two steps in the synthetic pathway were also performed under continuous flow conditions providing similar isolated product yields. As an alternative to the three-step protocol, a novel two-step route to the desired 4-(pyrazol-1-yl)carboxanilides was devised involving condensation of 4-bromophenylhydrazine with appropriate 1,3-dicarbonyl building blocks, followed by Pd-catalyzed Buchwald-Hartwig amidation with carboxylic acid amides.
- Obermayer, David,Glasnov, Toma N.,Kappe, C. Oliver
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p. 6657 - 6669
(2011/10/18)
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- 3,5-Bis(trifluoromethyl)pyrazoles: A novel class of NFAT transcription factor regulator
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A series of bis(trifiuoromethyl)pyrazoles (BTPs) has been found to be a novel inhibitor of cytokine production. Identified initially as inhibitors of IL-2 synthesis, the BTPs have been optimized in this regard and even inhibit IL-2 production with a 10-fold enhancement over cyclosporine in an ex vivo assay. Additionally, the BTPs show inhibition of IL-4, IL-5, IL-8, and eotaxin production. Unlike the IL-2 inhibitors, cyclosporine and FK506, the BTPs do not directly inhibit the dephosphorylation of NFAT by calcineurin.
- Djuric,Wiedeman,Zhou,Ballaron,Bauch,Chen,Chiou,Fey,Gauvin,Gubbins,Hsieh,Bamaung,Marsh,Mollison,Pong,Shaughnessy,Sheets,Smith,Trevillyan,Warrior,Wegner,Carter,Basha,Liu,Luly,Madar,Sciotti,Tu,Wagenaar
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p. 2975 - 2981
(2007/10/03)
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