Design and synthesis of an orally active matrix metalloproteinase inhibitor |
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| Authors: | Yamamoto Shingo Nakatani Shingo Ikura Masahiro Sugiura Tsuneyuki Nishita Yoshitaka Itadani Satoshi Ogawa Koji Ohno Hiroyuki Takahashi Kanji Nakai Hisao Toda Masaaki |
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| Institution: | Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan. |
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| Abstract: | A series of 4-(4-phenoxy)benzoylamino-4-methoxymethyloxymethyl butyric acid hydroxamates, which were derived from l-glutamic acid, were synthesized and evaluated as matrix metalloproteinase inhibitors. Most of the compounds listed in exhibited strong inhibitory activity against MMP-2 and MMP-9, as well as even stronger inhibitory activity against MMP-3, but showed relatively weak inhibition of MMP-1. Structure-activity relationships are discussed. |
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