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 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2015.04.023 |