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The synthesis, anti-inflammatory, and anti-microbial activity evaluation of new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives
Authors:Rajesh H. Tale  Atish H. Rodge  Girish D. Hatnapure  Ashish P. Keche  Kalpana M. Patil  Rajendra P. Pawar
Affiliation:1. Department of Chemistry, School of Chemical Sciences, Swam Ramanand Trith University (SRTM), Nanded, Maharashtra, India
2. Department of Chemistry, Udaygiri Mahavidyalaya, Udgir, Maharashtra, India
3. P. G. Research Centre, Deogiri College, Station Road, Aurangabad, Maharashtra, India
Abstract: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 6aj 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 6de and 6h exhibited relatively lower TNF-α and IL-6 inhibitory activity and found to be moderately potent anti-inflammatory agents. The compounds 6ce, 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.
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