Allylphenols as a new class of human 15‐lipoxygenase‐1 inhibitors. Issue 2 (6th October 2020)

• Record Type: Journal Article
• Authors: Alavi, Seyed Jamal; Seyedi, Seyed Mohammad; Saberi, Satar; Safdari, Hadi; Eshghi, Hossein; Sadeghian, Hamid
• Is Part Of: Drug development research. Volume 82:Issue 2(2021)
• Page Start: 259
• Page End: 266
• Publication Date: 2020-10-06
• Subjects: 15‐hLOX‐1 -- allylphenol -- Claisen rearrangement -- DPPH -- MBTH; Drug development -- Periodicals; Drugs -- Research -- Periodicals; 615.19
• DOI: 10.1002/ddr.21749
• Languages: English
• ISSNs: 0272-4391

Abstract

Abstract: In this study, a series of mono‐ and diallylphenol derivative were designed, synthesized, and evaluated as potential human 15‐lipoxygenase‐1 (15‐hLOX‐1) inhibitors. Radical scavenging potency of the synthetic allylphenol derivatives was assessed and the results were in accordance with lipoxygenase (LOX) inhibition potency. It was found that the electronic natures of allyl moiety and para substituents play the main role in radical scavenging activity and subsequently LOX inhibition potency of the synthetic inhibitors. Among the synthetic compounds, 2, 6‐diallyl‐4‐(hexyloxy)phenol (42 ) and 2, 6‐diallyl‐4‐aminophenol (47 ) showed the best results for LOX inhibition (IC50 = 0.88 and 0.80 μM, respectively).