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Eur J Med Chem ; 45(7): 3223-7, 2010 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-20430485

RESUMEN

This is the first report on aurones as a new class of drugs with anti-inflammatory and antimicrobial agents. A series of 2,2-bisaminomethylated aurone analogues (4a-j) were synthesized by Mannich reaction from 1,3,5-trimethoxybenzene in three steps. The structures of the newly synthesized compounds were confirmed by IR, (1)H NMR and mass spectral analysis. All the synthesized compounds were screened against the pro-inflammatory cytokines (TNF-alpha, IL-6) and antimicrobial (antibacterial and antifungal) activity. Compounds 4a, 4b, 4c, 4d, and 4e showed promising results against IL-6 at 10 microM concentration (74-100%). Compounds 4a, 4b and 4c were found to be active against TNF-alpha (76-100%) at 10 microM. Interestingly, all compounds have shown good antimicrobial activity. Compounds 4d, 4e and 4f showed excellent antimicrobial activity as compared with standard drugs.


Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Antiinflamatorios/síntesis química , Antiinflamatorios/farmacología , Benzofuranos/síntesis química , Benzofuranos/farmacología , Antiinfecciosos/química , Antiinflamatorios/química , Bacterias/efectos de los fármacos , Benzofuranos/química , Relación Dosis-Respuesta a Droga , Hongos/efectos de los fármacos , Interleucina-6/antagonistas & inhibidores , Pruebas de Sensibilidad Microbiana , Factor de Necrosis Tumoral alfa/antagonistas & inhibidores
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