Protein Information

Name 5 lipoxygenase
Synonyms 5 lipoxygenase; 5 LO; 5LPG; ALOX 5; ALOX5; Arachidonate 5 lipoxygenase; Arachidonate 5 lipoxygenase variant; LOG 5…

Compound Information

Name 1-naphthol
CAS 1-naphthalenol

Reference List

PubMed Abstract RScore(About this table)
8564418 Engman L, Stern D, Frisell H, Vessman K, Berglund M, Ek B, Andersson CM: Synthesis, antioxidant properties, biological activity and molecular modelling of a series of chalcogen analogues of the 5-lipoxygenase inhibitor DuP 654. Bioorg Med Chem. 1995 Sep;3(9):1255-62.

As judged by their ability to inhibit stimulated LTB4 biosynthesis in human neutrophils, compounds 1a-1d all turned out to be highly potent 5-lipoxygenase inhibitors with IC50-values ranging from 0.40 microM for 2-benzyl-1-naphthol (1a) to 0.063 microM for 2-phenyltellurenyl-1-naphthol (1d).
32(0,1,1,2) Details
2104936 Batt DG, Maynard GD, Petraitis JJ, Shaw JE, Galbraith W, Harris RR: 2-substituted-1-naphthols as potent 5-lipoxygenase inhibitors with topical antiinflammatory activity. J Med Chem. 1990 Jan;33(1):360-70.

To study the effects of structure on in vitro and in vivo activity, four general features of the molecules were varied: the 2-substituent, the 1-hydroxyl group, substitution on the naphthalene rings, and the 1,2-disubstituted naphthalene unit itself. 2-Benzyl-1-naphthol (5a, DuP 654) shows a very attractive profile of topical antiinflammatory activity and is currently in clinical trials as a topically applied antipsoriatic agent.
3(0,0,0,3) Details
2552761 Harris RR, Batt DG, Galbraith W, Ackerman NR: Topical anti-inflammatory activity of DuP 654, a 2-substituted 1-naphthol. . Agents Actions. 1989 Jun;27(3-4):297-9.

DuP 654, a 2-substituted 1-naphthol, is an exceptionally potent inhibitor of 5-lipoxygenase.
81(1,1,1,1) Details
8394724 Arenberger P, Raap A, Armah B, Kemeny L, Ruzicka T: The lipoxygenase inhibitor 2-phenylmethyl-1-naphthol (DuP 654) is a 12 (S)-hydroxyeicosatetraenoic acid receptor antagonist in the human epidermal cell line SCL-II. Skin Pharmacol. 1993;6(2):148-51.

Our results show that DuP 654, in addition to its 5-lipoxygenase inhibitory activity, exhibits 12-HETE receptor antagonist effect, and therefore may be of benefit in skin diseases with elevated 12-HETE levels.
1(0,0,0,1) Details
1439183 Kerr JS, Batt DG, Pinto DJ, Stampfli HF: An evaluation of 2-benzyl-1-naphthol (DuP 654) analogs as systemic anti-inflammatory agents. Res Commun Chem Pathol Pharmacol. 1992 Jul;77(1):77-86.

The compound is a potent 5-lipoxygenase inhibitor and exhibits inhibitory activity against lipopolysaccharide-stimulated release of interleukin-1 from human monocytes.
1(0,0,0,1) Details