Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents.
Bioorg Med Chem Lett
; 21(2): 644-51, 2011 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-21195617
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).
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
/
Compostos de Boro
/
Malária Falciparum
/
Antimaláricos
Limite:
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article