The synthesis, anti-inflammatory, and anti-microbial activity evaluation of new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives
A new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives were synthesized using simple three component condensation, reduction, and nucleophilic addition sequence in moderate to good yields. All the synthesized compounds 6a – j were evaluated for their anti-inflammatory [against t...
Gespeichert in:
Veröffentlicht in: | Medicinal chemistry research 2013-03, Vol.22 (3), p.1450-1455 |
---|---|
Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | A new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives were synthesized using simple three component condensation, reduction, and nucleophilic addition sequence in moderate to good yields. All the synthesized compounds
6a
–
j
were evaluated for their anti-inflammatory [against the pro-inflammatory cytokines (tumor necrosis factor-alpha, TNF-α and interleukin-6, IL-6)] and anti-microbial activity (anti-bacterial and anti-fungal). Among all the compound screened, the compound
6b
,
6f
, and
6j
were found to have promising anti-inflammatory activity, 74–83 % TNF-α and 91–96 % IL-6 inhibitory activity, respectively as compared to the standard dexamethasone (71 and 86 % inhibition) but at the MIC of 10 μM/ml. The compounds
6d
–
e
and
6h
exhibited relatively lower TNF-α and IL-6 inhibitory activity and found to be moderately potent anti-inflammatory agents. The compounds
6c
–
e
,
6g
, and
6i
were found to be promising anti-bacterial and anti-fungal agents and remarkably some of the new compounds, viz.
6d
and
6i
were found be more potent than the standard ciprofloxacin or miconazole. It is to be noted that this is the first report on the anti-inflammatory activity evaluation of novel 1,4-dihydropyridine urea derivatives against the important molecular target, TNF-α, and IL-6. |
---|---|
ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-012-0109-8 |