Please use this identifier to cite or link to this item:
Type
ArticleCopyright
Restricted access
Embargo date
2030-01-01
Collections
- IOC - Artigos de Periódicos [12828]
Metadata
Show full item record
SYNTHESIS AND ANTILEISHMANIAL EVALUATION OF 1-ARYL-4-(4,5-DIHYDRO-1H-IMIDAZOL-2-YL)-1H-PYRAZOLE DERIVATIVES
Author
Affilliation
Abstract
A series of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (4a-g) and 5-amino-1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (5a-g) were synthesized and evaluated in vitro against three Leishmania species: L. amazonensis, L. braziliensis and L. infantum (L. chagasi syn.). The cytotoxicity was assessed. Among the derivatives examined, six compounds emerged as the most active on promastigotes forms of L. amazonensis with IC(50) values ranging from 15 to 60 μM. The reference drug pentamidine presented IC(50)=10 μM. However, these new compounds were less cytotoxic than pentamidine. Based on these results, the more promising derivative 5d was tested further in vivo. This compound showed inhibition of the progression of cutaneous lesions in CBA mice infected with L. amazonensis relative to an untreated control.
Share