2. Academic Validation
  3. Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents

Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents

  • Bioorg Med Chem Lett. 2011 Jan 15;21(2):644-51. doi: 10.1016/j.bmcl.2010.12.034.
Yong-Kang Zhang 1,  Jacob J Plattner,  Yvonne R Freund,  Eric E Easom,  Yasheen Zhou,  Jiri Gut,  Philip J Rosenthal,  David Waterson,  Francisco-Javier Gamo,  Inigo Angulo-Barturen,  Min Ge,  Zhiya Li,  Lingchao Li,  Yong Jian,  Han Cui,  Hailong Wang,  Jian Yang
Affiliations

Affiliation

  • 1 Anacor Pharmaceuticals, Inc., 1020 E. Meadow Circle, Palo Alto, CA 94303, USA. yzhang@anacor.com
PMID: 21195617 DOI: 10.1016/j.bmcl.2010.12.034
Abstract

A series of boron-containing benzoxaborole compounds was designed and synthesized for a structure-activity relationship investigation surrounding 7-(HOOCCH(2)CH(2))-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering a new antimalarial treatment. Compound 1 demonstrates the best potency (IC(50)=26nM) against Plasmodium falciparum and has good drug-like properties, with low molecular weight (206.00), low ClogP (0.86) and high water solubility (750μg/mL at pH 7).

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