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Quinoline-Based Imidazole-Fused Heterocycles As New Inhibitors of 15-Lipoxygenase Publisher Pubmed



Dianat S1 ; Moghimi S2 ; Mahdavi M3 ; Nadri H4 ; Moradi A4 ; Firoozpour L3 ; Emami S5 ; Mouradzadegun A1 ; Shafiee A2 ; Foroumadi A2, 3
Authors

Source: Journal of Enzyme Inhibition and Medicinal Chemistry Published:2016


Abstract

A series of 2-chloro-quinoline-based imidazopyridines 6a–l and imidazothiazoles 6m–o bearing a bulky alkylamine side chain were synthesized as soybean 15-LOX inhibitors. The target compounds 6a–o were prepared via one-pot reaction of 2-chloroquinoline-3-carbaldehyde (3), heteroaromatic amidine 4, and alkyl isocyanides 5, in the presence of NH4Cl. All compounds showed significant anti-15-LOX activity (IC50 values ≤40 μM). Among the title compounds, the imidazo[2,1-b]thiazole derivative 6n bearing a tert-butylamine moiety showed the highest activity against soybean 15-LOX enzyme. © 2016 Informa UK Limited, trading as Taylor & Francis Group.
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