- A NEW PEPTIDE DEFORMYLASE INHIBITOR COMPOUND AND MANUFACTURING PROCESS THEREOF
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The present invention relates to the novel antibacterial compounds having potent antibacterial activity as inhibitors of peptide deformylase. This invention further relates to pharmaceutically acceptable salts thereof, to processes for their preparation, and to pharmaceutical compositions containing them as an active ingredient.
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Page/Page column 7
(2010/07/08)
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- A NEW PEPTIDE DEFORMYLASE INHIBITOR COMPOUND AND MANUFACTURING PROCESS THEREOF
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The present invention relates to the novel antibacterial compounds having potent antibacterial activity as inhibitors of peptide deformylase. This invention further relates to pharmaceutically acceptable salts thereof, to processes for their preparation, and to pharmaceutical compositions containing them as an active ingredient.
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Page/Page column 14-15
(2009/01/24)
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- N-(3-(4-Hydroxyphenyl)-propenoyl)-amino acid tryptamides as SIRT2 inhibitors
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A series of N-(3-(4-hydroxyphenyl)-propenoyl)-amino acid tryptamides was based on a previously reported new SIRT2 inhibitor from our group, and it was designed to study if the molecular size of the compound could be reduced. The most potent compounds, N-(3-(4-hydroxyphenyl)-propenoyl)-2-aminoisobutyric acid tryptamide and N-(3-(4-hydroxyphenyl)-propenoyl)-l-alanine tryptamide, were equipotent, 30% smaller in molecular weight, and slightly more selective (SIRT2/SIRT1) than the parent compound.
- Kiviranta, Paeivi H.,Leppaenen, Jukka,Rinne, Valtteri M.,Suuronen, Tiina,Kyrylenko, Olga,Kyrylenko, Sergiy,Kuusisto, Erkki,Tervo, Anu J.,Jaervinen, Tomi,Salminen, Antero,Poso, Antti,Wallen, Erik A.A.
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p. 2448 - 2451
(2008/02/03)
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- Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands
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The combination of the 3,5-bis(trifluoromethyl)phenyl group with a spirohydantoin motive as a central scaffold was the basis for the design of a combinatorial library targeted towards the neurokinin-1 receptor. A solution- and solid-phase procedure is described and binding affinities of representative compounds presented.
- Bleicher, Konrad H.,Wuethrich, Yves,De Boni, Maxime,Kolczewski, Sabine,Hoffmann, Torsten,Sleight, Andrew J.
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p. 2519 - 2522
(2007/10/03)
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