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Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates
Journal article   Peer reviewed

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

Roman N. Naumov, Siva S. Panda, Adel S. Girgis, Riham F. George, Michel Farhat and Alan R. Katritzky
Bioorganic & medicinal chemistry letters, Vol.25(11), pp.2314-2320
01/06/2015
PMID: 25937011

Abstract

Chemistry Chemistry, Medicinal Chemistry, Organic Life Sciences & Biomedicine Pharmacology & Pharmacy Physical Sciences Science & Technology
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. (C) 2015 Elsevier Ltd. All rights reserved.

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