(2016) Quinoline-based imidazole-fused heterocycles as new inhibitors of 15-lipoxygenase. Journal of Enzyme Inhibition and Medicinal Chemistry. pp. 205-209.
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Quinoline based imidazole fused heterocycles as new inhibitors of 15 lipoxygenase.pdf Download (953kB) |
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 imidazo2,1-bthiazole 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.
| Item Type: | Article |
|---|---|
| Keywords: | arachidonate 15 lipoxygenase; heterocyclic compound; imidazole; imidazole derivative; lipoxygenase inhibitor; quinoline; quinoline derivative, chemical structure; chemistry; dose response; enzymology; metabolism; molecular model; soybean; structure activity relation; synthesis, Arachidonate 15-Lipoxygenase; Dose-Response Relationship, Drug; Heterocyclic Compounds; Imidazoles; Lipoxygenase Inhibitors; Models, Molecular; Molecular Structure; Quinolines; Soybeans; Structure-Activity Relationship |
| Page Range: | pp. 205-209 |
| Journal or Publication Title: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Volume: | 31 |
| Publisher: | Taylor and Francis Ltd |
| Depositing User: | ms soheila Bazm |
| URI: | http://eprints.ssu.ac.ir/id/eprint/9708 |
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