{"id":1686,"date":"2020-09-04T15:40:28","date_gmt":"2020-09-04T06:40:28","guid":{"rendered":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/?p=1686"},"modified":"2020-09-04T15:43:10","modified_gmt":"2020-09-04T06:43:10","slug":"2019%e5%b9%b4%e5%ba%a6%e3%81%ae%e5%8f%96%e3%82%8a%e7%b5%84%e3%81%bf-2-2","status":"publish","type":"post","link":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/our-research\/2019%e5%b9%b4%e5%ba%a6%e3%81%ae%e5%8f%96%e3%82%8a%e7%b5%84%e3%81%bf-2-2\/","title":{"rendered":"2019\u5e74\u5ea6\u306e\u53d6\u308a\u7d44\u307f (#2\/2)"},"content":{"rendered":"\n<h3>Divergent syntheses of new artificial glutamate analogs<\/h3>\n<p>\u4e2d\u67a2\u795e\u7d4c\u30b7\u30ca\u30d7\u30b9\u5f8c\u7d42\u672b\u306b\u3066\u30a4\u30aa\u30f3\u30c1\u30e3\u30cd\u30eb\u578b\u30b0\u30eb\u30bf\u30df\u30f3\u9178\u53d7\u5bb9\u4f53\uff08iGluR\uff09\u306f\u8208\u596e\u6027\u306e\u795e\u7d4c\u4f1d\u9054\u3092\u62c5\u3063\u3066\u3044\u308b\u3002iGluR\u306f\u30ea\u30ac\u30f3\u30c9\u7d50\u5408\u30c9\u30e1\u30a4\u30f3\uff08LBD\uff09\u3092\u6709\u3057\u3066\u304a\u308a\u3001\u30ea\u30ac\u30f3\u30c9\u304c\u7d50\u5408\u3059\u308b\u3053\u3068\u306b\u3088\u308a\u6a5f\u80fd\u3092\u767a\u73fe\u3059\u308b\u3053\u3068\u304c\u660e\u3089\u304b\u306b\u306a\u3063\u3066\u3044\u308b\u304c\u3001\u5206\u5b50\u30ec\u30d9\u30eb\u3067\u306e\u8a73\u7d30\u306a\u30e1\u30ab\u30cb\u30ba\u30e0\u89e3\u660e\u306b\u306f\u81f3\u3063\u3066\u3044\u306a\u3044\u3002<\/p>\n<p>IKM\u2013159\u306f\u6d77\u6d0b\u6027\u7531\u6765\u306e\u5929\u7136\u7269\u3067\u3042\u308b\u30c0\u30a4\u30b7\u30cf\u30fc\u30d9\u30a4\u30f3\u3068\u30ab\u30a4\u30cb\u30f3\u9178\u3092\u30e2\u30c1\u30fc\u30d5\u306b\u5f53\u7814\u7a76\u5ba4\u3067\u4eba\u5de5\u7684\u306b\u958b\u767a\u3055\u308c\u305f\u5316\u5408\u7269\u3067\u3001\u751f\u7269\u6d3b\u6027\u8a66\u9a13\u3067\u306f\u30de\u30a6\u30b9\u306e\u81ea\u767a\u7684\u884c\u52d5\u3092\u6291\u5236\u3057\u305f\uff08Scheme 1\uff09\u3002\u96fb\u6c17\u751f\u7406\u5b66\u7684\u624b\u6cd5\u3092\u7528\u3044\u305fin vitro\u8a66\u9a13\u3067\u306f\u3001AMPA\u53d7\u5bb9\u4f53\u3092\u30b5\u30d6\u30bf\u30a4\u30d7\u9078\u629e\u7684\u306b\u963b\u5bb3\u3059\u308b\u3053\u3068\u304c\u767a\u898b\u3055\u308c\u305f\u3002IKM\u2013159\uff086\u54e1\u74b0\u30a2\u30df\u30f3\uff09\u306eC\u74b0\u90e8\u985e\u7e01\u4f53\u3067\u3042\u308bTKM\u2013107\uff087\u54e1\u74b0\u30a2\u30df\u30f3\uff093\u3001MC\u201327\uff086\u54e1\u74b0\u30a8\u30fc\u30c6\u30eb\uff09\u3082\u540c\u69d8\u306bin 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sizes=\"auto, (max-width: 300px) 100vw, 300px\" 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wp-image-1690\" src=\"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/2-300x159.png\" alt=\"\" width=\"300\" height=\"159\" srcset=\"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/2-300x159.png 300w, http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/2-1024x543.png 1024w, http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/2-768x407.png 768w, http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/2-1536x815.png 1536w, http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/2-2048x1086.png 2048w\" sizes=\"auto, (max-width: 300px) 100vw, 300px\" \/><\/p>\n<h4>(2R)\u2013TKM\u201338 (1)\u306e\u5408\u6210<\/h4>\n<p>\u30aa\u30ad\u30b5\u30ce\u30eb\u30dc\u30eb\u30cd\u30f34\u306b\u5e38\u6cd5\u3092\u7528\u3044\u3066N\u2013pentenyl TFA amide\u57fa\u3092\u5c0e\u5165\u3057\u305f\uff08Scheme 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(1)\u306e\u5408\u6210\u306b\u6210\u529f\u3057\u305f\u3002\u7dcf\u53ce\u7387\u306f(Z)\u20132\u2013iodoacrylic acid\u304b\u308910\u6bb5\u968e\u30671.9%\u3067\u3042\u3063\u305f\u3002(2R)\u2013TKM\u201338\u30925 mg\/mL\u306e\u6fc3\u5ea6\u3067\u30de\u30a6\u30b9\u306e\u8133\u5ba4\u5185\u306b10 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src=\"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/3-300x142.png\" alt=\"\" width=\"300\" height=\"142\" srcset=\"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/3-300x142.png 300w, http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/3-1024x485.png 1024w, http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/3-768x364.png 768w, http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/3-1536x727.png 1536w, http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-content\/uploads\/2020\/09\/3-2048x970.png 2048w\" sizes=\"auto, (max-width: 300px) 100vw, 300px\" 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(3a)\u306e\u5408\u6210\u3092\u9054\u6210\u3057\u305f\uff08\u8a0814\u6bb5\u968e\u3001\u7dcf\u53ce\u738712%\uff09\u3002\u307e\u305f\u3001\u30db\u30e2\u30a2\u30ea\u30eb\u30a2\u30eb\u30b3\u30fc\u30eb7\u306b\u5bfe\u3057\u3066\u30aa\u30af\u30c6\u30ce\u30f3\u30844\u2013\u30e1\u30c8\u30ad\u30b7\u30d5\u30a7\u30cb\u30eb\u30d3\u30cb\u30eb\u30b1\u30c8\u30f3\u3092\u5c0e\u5165\u3057\u3001\u30aa\u30ad\u30b5\u30de\u30a4\u30b1\u30eb\u53cd\u5fdc\u3092\u884c\u3046\u3053\u3068\u3067\u3001\u5bfe\u5fdc\u3059\u308b\u30b8\u30aa\u30ad\u30b5\u30f319b\u306819c\u3092\u5f97\u308b\u3053\u3068\u306b\u3082\u6210\u529f\u3057\u3001\u76f4\u9396\u306e\u8102\u80aa\u65cf\u3084\u82b3\u9999\u65cf\u5316\u5408\u7269\u306b\u5bfe\u3057\u3066\u3082\u672c\u53cd\u5fdc\u3092\u9069\u7528\u3067\u304d\u308b\u3053\u3068\u3092\u793a\u305b\u305f\u3002\u305d\u308c\u305e\u308c\u3001\u8131\u4fdd\u8b77\u3059\u308b\u3053\u3068\u3067\u3001TKM\u201386\uff083b\u3001\u8a0814\u6bb5\u968e\u3001\u7dcf\u53ce\u73878.8%\uff09\u3068TKM\u201399\uff083c\u3001\u8a0814\u6bb5\u968e\u3001\u7dcf\u53ce\u73871.7%\uff09\u3068\u540d\u4ed8\u3051\u305f\u985e\u7e01\u4f53\u3082\u5408\u6210\u3057\u305f\u3002<\/p>\n<p>TKM\u201350\u30925 mg\/mL\u306e\u6fc3\u5ea6\u3067\u30de\u30a6\u30b9\u306e\u8133\u5ba4\u5185\u306b10 uL\u6295\u4e0e\u3057\u3001\u52b9\u679c\u3092\u89b3\u5bdf\u3057\u305f\uff08\u672a\u767a\u8868\u306e\u305f\u3081\u8a73\u7d30\u306f\u975e\u516c\u958b\uff09\u3002\u3053\u306e\u3088\u3046\u306b\u3001\u672c\u7814\u7a76\u3067\u306fC7\u4f4d\u306b\u7f6e\u63db\u57fa\u3092\u6301\u3063\u305f\u6d3b\u6027\u306e\u3042\u308b\u30b0\u30eb\u30bf\u30df\u30f3\u9178\u985e\u7e01\u4f53\u306e\u5408\u6210\u306b\u6210\u529f\u3057\u305f\u306e\u3067\u3001\u73fe\u5728\u306f\u3053\u306e\u4f4d\u7f6e\u306b\u5149\u89aa\u548c\u6027\u6a19\u8b58\u57fa\u3092\u5c0e\u5165\u3059\u308b\u3053\u3068\u3092\u691c\u8a0e\u3057\u3066\u3044\u308b\u3002<\/p>\n<h4>\u53c2\u8003\u6587\u732e<\/h4>\n<ol>\n<li>M. B. Gill et al., Br. J. Pharmacol., 2010, 160, 1417-1429.<\/li>\n<li>M. Oikawa et al., J. Synth. Org. Chem. Jpn., 2020, in press.<\/li>\n<li>S. Tsukamoto et al., Heterocycles, 2020, 101, 91-98.<\/li>\n<li>L. Juknaite et al., J. Med. Chem., 2013, 56, 2283-2293.<\/li>\n<li>M. Chiba et al., Bioorg. Med. Chem. Lett., 2015, 25, 1869-1871.<\/li>\n<\/ol>\n","protected":false},"excerpt":{"rendered":"Divergent syntheses of new artificial glutamate analogs \u4e2d\u67a2\u795e\u7d4c\u30b7\u30ca\u30d7\u30b9\u5f8c\u7d42\u672b\u306b\u3066\u30a4\u30aa\u30f3\u30c1\u30e3\u30cd\u30eb\u578b\u30b0\u30eb\u30bf\u30df\u30f3\u9178\u53d7\u5bb9\u4f53\uff08iGluR\uff09\u306f\u8208\u596e\u6027\u306e\u795e\u7d4c\u4f1d\u9054\u3092\u62c5\u3063\u3066\u3044\u308b\u3002i &#8230;","protected":false},"author":6,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[21],"tags":[],"class_list":["post-1686","post","type-post","status-publish","format-standard","hentry","category-our-research"],"_links":{"self":[{"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/posts\/1686","targetHints":{"allow":["GET"]}}],"collection":[{"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/users\/6"}],"replies":[{"embeddable":true,"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/comments?post=1686"}],"version-history":[{"count":4,"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/posts\/1686\/revisions"}],"predecessor-version":[{"id":1694,"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/posts\/1686\/revisions\/1694"}],"wp:attachment":[{"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/media?parent=1686"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/categories?post=1686"},{"taxonomy":"post_tag","embeddable":true,"href":"http:\/\/oiklab.sci.yokohama-cu.ac.jp\/wp\/wp-json\/wp\/v2\/tags?post=1686"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}