- Use of functionalized onium salts as a soluble support for organic synthesis
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The invention relates to the use of a onium salt functionalized by at least one organic function, as a soluble support, in the presence of at least one organic solvent, for organic synthesis of a molecule, in a homogenous phase, by at least one transformation of said organic function. The onium salt enables the synthesized molecule to be released. The onium salt is present in liquid or solid form at room temperature and corresponds to formula A1+, X1?, wherein A1+ represents a cation and X1? represents an anion.
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Page/Page column 56
(2010/11/25)
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- Design and synthesis of novel metalloproteinase inhibitors
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A series of N-benzoyl 4-aminobutyric acid hydroxamate analogs were synthesized and evaluated as matrix metalloproteinase inhibitors. Synthetic work was focused on the chemical modification of the 4-aminobutyric acid part using easily available starting materials. As such, chemical modification was carried out using commercially available starting materials such as 4-aminobutyric acid, (+)- and (-)-malic acid, and d- and l-glutamic acid derivatives. Among the compounds tested, N-[4-(benzofuran-2-yl)benzoyl] 4-amino-4S-hydroxymethylbutyric acid hydroxamates derived from l-glutamic acid demonstrated more potent inhibitory activity against MMP-2 and MMP-9 compared with the corresponding 2S-hydroxy analogs or 3S-hydroxy analogs, respectively, which were derived from (-)-malic acid. Structure-activity relationship study is presented.
- Nakatani, Shingo,Ikura, Masahiro,Yamamoto, Shingo,Nishita, Yoshitaka,Itadani, Satoshi,Habashita, Hiromu,Sugiura, Tsuneyuki,Ogawa, Koji,Ohno, Hiroyuki,Takahashi, Kanji,Nakai, Hisao,Toda, Masaaki
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p. 5402 - 5422
(2007/10/03)
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