Synthesis and structure–activity relationships of novel benzoxaboroles as a new class of antimalarial agents
✍ Scribed by Yong-Kang Zhang; 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
- Publisher
- Elsevier Science
- Year
- 2011
- Tongue
- English
- Weight
- 801 KB
- Volume
- 21
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
A series of boron-containing benzoxaborole compounds was designed and synthesized for a structureactivity 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 = 26 nM) against Plasmodium falciparum and has good drug-like properties, with low molecular weight (206.00), low ClogP (0.86) and high water solubility (750 lg/mL at pH 7).
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