Synthesis of new quinazolin-2,4-diones as anti-Leishmania mexicana agents.
Mol Divers
; 20(4): 821-828, 2016 Nov.
Article
in En
| MEDLINE
| ID: mdl-27531196
ABSTRACT
The quinazolin-2,4-dione moiety is found in many compounds with important biological activities making it a target for its synthesis. In this work, a one-pot three-step synthesis of new quinazolin-2,4-diones from phthalic anhydrides and their activity against Leishmania mexicana are described. The new quinazolin-2,4-diones were isolated with yields in the range of 32-70 %. All compounds displayed lower cytotoxicity in RAW 264.7 macrophage over miltefosine. Compound 6,7-dichloro-3-phenylquinazoline-2,4(1H,3H)-dione (6e) displayed an attractive profile which includes anti-Leishmania mexicana activity ([Formula see text] [Formula see text]M), much lower cytotoxic activity ([Formula see text] [Formula see text]M) and a high selective index ([Formula see text]) proving to be superior to miltefosine.
Key words
Search on Google
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Leishmania mexicana
/
Quinazolinones
/
Antiprotozoal Agents
Limits:
Animals
Country/Region as subject:
Mexico
Language:
En
Journal:
Mol Divers
Journal subject:
BIOLOGIA MOLECULAR
Year:
2016
Type:
Article
Affiliation country:
Mexico