کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1371056 | 981838 | 2011 | 8 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: 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](/preview/png/1371056.png)
A series of boron-containing benzoxaborole compounds was designed and synthesized for a structure–activity relationship investigation surrounding 7-(HOOCCH2CH2)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering a new antimalarial treatment. Compound 1 demonstrates the best potency (IC50 = 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 μg/mL at pH 7).
A series of boron-containing benzoxaborole compounds was designed and synthesized for a SAR investigation for discovering a new antimalarial treatment. Compound 1 demonstrates the best potency (IC50 = 26 nM) against Plasmodium falciparum and has good drug-like properties, with low molecular weight, low ClogP and high water solubility.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 2, 15 January 2011, Pages 644–651