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Synthesis and antibacterial evaluation of a novel tricyclic oxaborole-fused fluoroquinolone. 2013
Xianfeng Li, and
Yong-Kang Zhang, and
Jacob J Plattner, and
Weimin Mao, and
M R K Alley, and
Yi Xia, and
Vincent Hernandez, and
Yasheen Zhou, and
Charles Z Ding, and
Jinpeng Li, and
Zhijun Shao, and
Hongwei Zhang, and
Musheng Xu
Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA. xli@anacor.com
We have designed and synthesized a novel class of compounds based on fluoroquinolone antibacterial prototype. The design concept involved the replacement of the 3-carboxylic acid in ciprofloxacin with an oxaborole-fused ring as an acid-mimicking group. The synthetic method employed in this work provides a good example of incorporating boron atom in complex molecules with multiple functional groups. The antibacterial activity of the newly synthesized compounds has been evaluated.
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