吲哚喹啉类似物抗耐甲氧西林金黄色葡萄球菌的构效关系
Structure-activity relationship of indoloquinoline analogs anti-MRSA.
作者信息
Zhao Min, Kamada Tomonori, Takeuchi Aya, Nishioka Hiromi, Kuroda Teruo, Takeuchi Yasuo
机构信息
Faculty of Pharmaceutical Sciences, Okayama University, Kitaku-Tsushima-naka 1-1-1, Okayama 700-8530, Japan.
Faculty of Pharmaceutical Sciences, Okayama University, Kitaku-Tsushima-naka 1-1-1, Okayama 700-8530, Japan.
出版信息
Bioorg Med Chem Lett. 2015 Dec 1;25(23):5551-4. doi: 10.1016/j.bmcl.2015.10.058. Epub 2015 Oct 21.
Indolo[3,2-b]quinoline analogs (3a-3s), 4-(acridin-9-ylamino) phenol hydrochloride (4), benzofuro[3,2-b]quinoline (3t), indeno[1,2-b]quinolines (3u and 3v) have been synthesized. Those compounds were found to exhibit anti-bacterial activity towards Methicillin-resistant Staphylococcus aureus (anti-MRSA activity). Structure-activity relationship studies were conducted that indoloquinoline ring, benzofuroquinoline ring and 4-aminophenol group are essential structure for anti-MRSA activity.
已合成吲哚并[3,2 - b]喹啉类似物（3a - 3s）、4 -（吖啶 - 9 - 基氨基）苯酚盐酸盐（4）、苯并呋喃并[3,2 - b]喹啉（3t）、茚并[1,2 - b]喹啉（3u和3v）。发现这些化合物对耐甲氧西林金黄色葡萄球菌具有抗菌活性（抗MRSA活性）。进行了构效关系研究，结果表明吲哚喹啉环、苯并呋喃喹啉环和4 - 氨基苯酚基团是抗MRSA活性的关键结构。
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