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Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jan 15; Vol. 21 (2), pp. 644-51. Date of Electronic Publication: 2010 Dec 10. - Publication Year :
- 2011
-
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).<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Antimalarials chemical synthesis
Boron Compounds chemical synthesis
Cell Line
Cell Survival drug effects
Humans
Parasitic Sensitivity Tests
Structure-Activity Relationship
Antimalarials chemistry
Antimalarials pharmacology
Boron Compounds chemistry
Boron Compounds pharmacology
Malaria, Falciparum drug therapy
Plasmodium falciparum drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21195617
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.12.034