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

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Abstract

Abstract 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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Naumov, R. N., Panda, S. S., Girgis, A. S., George, R. F., Farhat, M., & Katritzky, A. R. (2015). Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates. Bioorganic and Medicinal Chemistry Letters, 25(11), 2314–2320. https://doi.org/10.1016/j.bmcl.2015.04.023

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