title: Synthesis and antibacterial evaluation of a novel tricyclic oxaborole-fused fluoroquinolone.
abstract: 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.
authors: Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA. xli@anacor.com
authors: Xianfeng
authors: X
authors: Li
authors: Yong-Kang
authors: YK
authors: Zhang
authors: Jacob J
authors: JJ
authors: Plattner
authors: Weimin
authors: W
authors: Mao
authors: M R K
authors: MR
authors: Alley
authors: Yi
authors: Y
authors: Xia
authors: Vincent
authors: V
authors: Hernandez
authors: Yasheen
authors: Y
authors: Zhou
authors: Charles Z
authors: CZ
authors: Ding
authors: Jinpeng
authors: J
authors: Li
authors: Zhijun
authors: Z
authors: Shao
authors: Hongwei
authors: H
authors: Zhang
authors: Musheng
authors: M
authors: Xu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001896:Boron Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis / Q000494:pharmacology; D002939:Ciprofloxacin / Q000737:chemistry / Q000494:pharmacology; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D001896:Boron Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D024841:Fluoroquinolones; D002939:Ciprofloxacin