- Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists
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N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high-throughput screen (HTS) of a subset of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent sta
- Kindon, Nicholas,Andrews, Glen,Baxter, Andrew,Cheshire, David,Hemsley, Paul,Johnson, Timothy,Liu, Yu-Zhen,McGinnity, Dermot,McHale, Mark,Mete, Antonio,Reuberson, James,Roberts, Bryan,Steele, John,Teobald, Barry,Unitt, John,Vaughan, Deborah,Walters, Iain,Stocks, Michael J.
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Read Online
- Peptide deformylase inhibitors
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The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
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(2014/12/09)
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- Necrosulfonamide inhibits necroptosis by selectively targeting the mixed lineage kinase domain-like protein
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Through high-throughput screening of 200000 compounds and subsequent structure-activity relationship (SAR) studies we identified necrosulfonamide (NSA) as a potent small molecule inhibitor for necroptosis, induced by a combination of TNF-a, Smac mimetic, and z-VAD-fmk (T/S/Z). Applying a forward chemical genetic approach, we utilized an NSA based chemical probe to further reveal that NSA selectively targeted the Mixed Lineage Kinase Domain-like Protein (MLKL) to block the necrosome formation.
- Liao, Daohong,Sun, Liming,Liu, Weilong,He, Sudan,Wang, Xiaodong,Lei, Xiaoguang
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supporting information
p. 333 - 337
(2014/03/21)
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- PEPTIDE DEFORMYLASE INHIBITORS
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The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhi-bition of bacterial peptide deformylase (PDF) activity
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Page/Page column
(2014/02/15)
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- Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
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This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
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- A new route to aminodiazines via metalation reaction. Synthesis of an aza analogue of Nevirapine: Diazines XV
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A new route to aminodiazines is reported, the ortho-directed lithiation of diazines is used, followed by reaction with tosyl azide as an electrophile. The reduction of the azido or tetrazolo compounds obtained was achieved and led to the expected amines. This methodology has allowed the synthesis of new aminodiazines and an improvement in the yield of various aminodiazines previously described. This reaction was used for the preparation of an aza analogue of Nevirapine.
- Plé, Nelly,Turck, Alain,Couture, Karine,Quéguiner, Guy
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p. 838 - 842
(2007/10/03)
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- Synthesis of Derivatives of Pyrazinopyridimidin-4-ones
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3-Alkoxy-2-aminopyrazines have been condensed with ethyl ethoxymethylenemalonate and isopropylidene methoxymethylenemalonate to afford 9-alkoxypyrazinopyrimidin-4-ones substituted in the first case by an ethoxycarbonyl group at 3 position.
- Dennin, F.,Blondeau, D.,Sliwa, H.
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p. 1639 - 1643
(2007/10/02)
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