Anti-leishmanial and structure-activity relationship of ring substituted 3-phenyl-1-(1, 4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives
Mem. Inst. Oswaldo Cruz
;
103(8): 778-780, Dec. 2008. tab
Article
in English
| LILACS
| ID: lil-502297
ABSTRACT
A series of ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives were synthesized and tested for in vitro leishmanicidal activity against amastigotes of Leishmania amazonensis in axenical cultures and murine infected macrophages. Structure-activity relationships demonstrated the importance of a radical methoxy at position R3', R4' and R5'. (2E)-3-(3,4,5-trimethoxy-phenyl)-1-(3,6,7-trimethyl-1,4-dioxy-quinoxalin-2-yl)-propenone was the most active. Cytotoxicity on macrophages revealed that this product was almost six times more active than toxic.
Full text:
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Index:
LILACS (Americas)
Main subject:
Quinoxalines
/
Leishmania mexicana
/
Cyclic N-Oxides
/
Antiprotozoal Agents
Limits:
Animals
Language:
English
Journal:
Mem. Inst. Oswaldo Cruz
Journal subject:
Tropical Medicine
/
Parasitology
Year:
2008
Type:
Article
Affiliation country:
France
/
Peru
/
Spain
Institution/Affiliation country:
Universidad Peruana Cayetano Heredia/PE
/
University of Navarra/ES
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