7位含芳香杂环的异噻唑并喹诺酮类化合物的生物学评价：对耐甲氧西林金黄色葡萄球菌有效的一系列强效抗菌剂的体外活性
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
作者信息
Wiles Jason A, Song Yongsheng, Wang Qiuping, Lucien Edlaine, Hashimoto Akihiro, Cheng Jijun, Marlor Christopher W, Ou Yangsi, Podos Steven D, Thanassi Jane A, Thoma Christy L, Deshpande Milind, Pucci Michael J, Bradbury Barton J
机构信息
Achillion Pharmaceuticals, Inc., 300 George Street, New Haven, CT 06511-6653, USA.
出版信息
Bioorg Med Chem Lett. 2006 Mar 1;16(5):1277-81. doi: 10.1016/j.bmcl.2005.11.064. Epub 2005 Dec 7.
We synthesized a diverse series of 9H-isothiazolo[5,4-b]quinoline-3,4-diones containing heteroaromatic groups at the 7-position via palladium-catalyzed cross-coupling. Many of these compounds demonstrated potent antistaphylococcal activity (MICs 2 microg/mL) against a multi-drug-resistant strain (ATCC 700699) and low cytotoxic activity (CC(50)>100 microM) against the human cell line Hep2 (laryngeal carcinoma).
我们通过钯催化交叉偶联反应合成了一系列多样的7位含有杂芳基的9H-异噻唑并[5,4-b]喹啉-3,4-二酮。这些化合物中的许多对多重耐药菌株（ATCC 700699）表现出强效的抗葡萄球菌活性（MICs为2微克/毫升），对人喉癌细胞系Hep2的细胞毒性活性较低（CC(50)>100微摩尔）。
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