螺萘啶酮哌啶类化合物作为金黄色葡萄球菌和大肠杆菌烯酰-ACP还原酶（FabI）的抑制剂
Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI).
作者信息
Sampson Peter B, Picard Christine, Handerson Sean, McGrath Teresa E, Domagala Megan, Leeson Andrew, Romanov Vladimir, Awrey Donald E, Thambipillai Dhushy, Bardouniotis Elias, Kaplan Nachum, Berman Judd M, Pauls Henry W
机构信息
Affinium Pharmaceuticals Inc. 1243 Islington Ave., Suite 600, Toronto, Ontario, Canada M8X 1Y9.
出版信息
Bioorg Med Chem Lett. 2009 Sep 15;19(18):5355-8. doi: 10.1016/j.bmcl.2009.07.129. Epub 2009 Aug 6.
Spiropiperidine naphthyridinone inhibitors of Staphylococcus aureus and Escherichia coli FabI have been prepared. Compounds 14a and 14c were identified as having sub-nanomolar E. coli FabI activity and are among the most potent FabI inhibitors yet described. The structural model of 14a bound to E. coli FabI is shown.
已制备出金黄色葡萄球菌和大肠杆菌FabI的螺哌啶萘啶酮抑制剂。化合物14a和14c被鉴定为具有亚纳摩尔级的大肠杆菌FabI活性，是迄今所描述的最有效的FabI抑制剂之一。展示了与大肠杆菌FabI结合的14a的结构模型。
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