Infection Innovative Medicines, AstraZeneca R&D Boston, Waltham, MA 02451, USA.
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5432-5. doi: 10.1016/j.bmcl.2011.06.126. Epub 2011 Jul 2.
An SAR survey at the C-6 benzoxazinone position of a novel scaffold which inhibits bacterial type IIa topoisomerase demonstrates that a range of small electron donating groups (EDG) and electron withdrawing groups (EWG) are tolerated for antibacterial activity. Cyano was identified as a preferred substituent that affords good antibacterial potency while minimizing hERG cardiac channel activity.
一种新型骨架的 C-6 苯并恶嗪酮位置的 SAR 研究表明，一系列的小供电子基团（EDG）和吸电子基团（EWG）可被耐受以保持抗菌活性。氰基被鉴定为一种优选取代基，可提供良好的抗菌效力，同时最小化 hERG 心脏通道活性。
