Structure--activity relationships of azasugar-based MMP/ADAM inhibitors.
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Moriyama H, Tsukida T, Inoue Y, Kondo H, Yoshino K, Nishimura S
Structure--activity relationships of azasugar-based MMP/ADAM inhibitors.
Bioorg Med Chem Lett. 2003 Aug 18;13(16):2737-40.
- PubMed ID
- 12873504 [ View in PubMed]
- Abstract
In order to investigate structure-activity relationships of azasugar series toward metalloproteinases, we synthesized and evaluated several azasugar-based compounds. As a result, it was found that 4-phenoxybenzene derivative 3 having 2R,3R,4R,5S-configurations exhibited most potent inhibitory activities against matrix metalloproteinase-1, -3 and -9 and TACE.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Marimastat Interstitial collagenase Ki (nM) 1.1 N/A N/A Details Marimastat Stromelysin-1 Ki (nM) 84 N/A N/A Details