High selective leishmanicidal activity of 3-hydroxy-2-methylene-3-(4-bromophenyl)propanenitrile and analogous compounds.
Eur J Med Chem
; 42(1): 99-102, 2007 Jan.
Article
en En
| MEDLINE
| ID: mdl-17010481
ABSTRACT
Sixteen not new aromatic compounds were prepared by one-pot reaction i.e. through Baylis-Hillman reaction and were the first time evaluated against promastigote Leishmania amazonensis and infected mammalian cells. Most of the compounds were selectively more active against amastigotes than the reference drug sodium stibogluconate (Pentostam, IC(50)=44.7 microM). We found that 3-hydroxy-2-methylene-3-(4-bromophenyl) propanenitrile (13) was the most active (IC(50)=12.5 microM) and safer compound (0.0 (0.9); % macrophage LDH release), being the lead compound.
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Bases de datos:
MEDLINE
Asunto principal:
Tripanocidas
/
Leishmania
/
Nitrilos
Límite:
Animals
Idioma:
En
Revista:
Eur J Med Chem
Año:
2007
Tipo del documento:
Article
País de afiliación:
Brasil