- SUBSTITUTED PYRAZINE DITHIOL REDUCING AGENTS
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Substituted dithiol pyrazine compounds useful as reducing agents in biologically relevant media having formula: where variables are defined herein and corresponding oxidized pyrazine dithianes. Reducing agents useful to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins, and other biological molecules. Reducing agents useful to regulate protein function in proteins in which a sulfhydryl group is associated with biological activity. Reducing agents useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. S-acylated dithiol pyrazine compounds, where R3 is an acyl group, are selectively activated as reducing agents by removal of the S-acyl groups enzymatically or chemically. Dithiol pyrazine reducing agents and corresponding S-acylated dithiol pyrazines, immobilized on surfaces or conjugated to other chemical species, are provided.
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Paragraph 0174-0176
(2016/01/25)
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- Pyrazine-derived disulfide-reducing agent for chemical biology
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For fifty years, dithiothreitol (DTT) has been the preferred reagent for the reduction of disulfide bonds in proteins and other biomolecules. Herein we report on the synthesis and characterization of 2,3-bis(mercaptomethyl)pyrazine (BMMP), a readily accessible disulfide-reducing agent with reactivity under biological conditions that is markedly superior to DTT and other known reagents. This journal is the Partner Organisations 2014.
- Lukesh, John C.,Wallin, Kelly K.,Raines, Ronald T.
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supporting information
p. 9591 - 9594
(2014/08/18)
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- HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The present invention related to novel heterocyclic amide compounds of Formula 1: as disclosed herein or a pharmaceutically accept able salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosedare compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease
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Page/Page column 88-89
(2009/03/07)
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- AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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Page/Page column 36
(2010/11/28)
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- The syntheses of pyrazino-containing sultines and their application in Diels-Alder reactions with electron-poor olefins and [60]fullerene
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The Diels-Alder reactions of heterocyclic o-quinodimethanes, generated in situ from 6,7-disubstituted quinoxalino[2,3-d]-[1,2λ4]oxathiine 2-oxides (6a-c), 2,3-disubstituted-8,9-dihydro-6H-8λ 4-[1,2]oxathiino[4,5-g]quinoxalin-8-one (7a-c) (sultines), and pyrazinosultine (22), with electron-poor olefins and [60]fullerene are described. The heterocyclic-fused sultines 7a-c and 22 are readily prepared from the corresponding dibromides 9a-c and 24 with the commercially available Rongalite (sodium formaldehyde sulfoxylate). When heated in the presence of electron-poor dienophiles and [60]fullerene, all of the sultines underwent extrusion of SO2, and the resulting heterocyclic o-quinodimethanes (3a-d, 4a-c, and 25) were intercepted as the 1:1 adducts in good to excellent yields. The temperature-dependent 1H NMR spectra of fullerene derivatives 31-38 show a dynamic process for the methylene protons. The activation free energies (ΔGc?) determined for the boat-to-boat inversion of these pyrazino-containing C60 compounds (31-34 and 38) are found to be in the range of 14.1-14.8 kcal/mol, but they are in the range of 15.2 to >17.1 kcal/mol for adducts 35-37. The activation free energies (ΔGC?) are significantly affected by (1) the orientations and (2) the substituents of the quinoxaline rings and (3) the extended benzannulation in the arenes of C60 adducts (see Table 2), which implies that both electronic interactions and steric effects between the aromatic addends and C60 are important. Tautomerization of methylquinoxaline to its enamine is invoked as a rationalization for the lowering of ΔGC? in some of the fulleroadducts.
- Liu, Jing-Horng,Wu, An-Tai,Huang, Ming-Hwei,Wu, Chein-Wei,Chung, Wen-Sheng
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p. 3395 - 3403
(2007/10/03)
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