Synthesis and QSAR study of novel anti-inflammatory active mesalazine–metronidazole conjugates

[Display omitted] Novel, mesalazine, metronidazole conjugates 6a–e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2015-06, Vol.25 (11), p.2314-2320
Hauptverfasser: Naumov, Roman N., Panda, Siva S., Girgis, Adel S., George, Riham F., Farhat, Michel, Katritzky, Alan R.
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Sprache:eng
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Zusammenfassung:[Display omitted] Novel, mesalazine, metronidazole conjugates 6a–e with amino acid linkers were synthesized utilizing benzotriazole chemistry. Biological data acquired for all the novel bis-conjugates showed (a) some bis-conjugates exhibit comparable anti-inflammatory activity with parent drugs and (b) the potent bis-conjugates show no visible stomach lesions. 3D-pharmacophore and 2D-QSAR modeling support the observed bio-properties.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.04.023