3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1. Issue 15 (1st August 2015)

• Record Type: Journal Article
• Authors: Pelcman, Benjamin; Sanin, Andrei; Nilsson, Peter; No, Kiyo; Schaal, Wesley; Öhrman, Sara; Krog-Jensen, Christian; Forsell, Pontus; Hallberg, Anders; Larhed, Mats; Boesen, Thomas; Kromann, Hasse; Vogensen, Stine Byskov; Groth, Thomas; Claesson, Hans-Erik
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 15(2015)
• Page Start: 3024
• Page End: 3029
• Publication Date: 2015-08-01
• Subjects: 15-Lipoxygenase -- Inhibitors -- Arachidonic acid -- Pyrazole -- Triazole -- Benzoxazole; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.05.004
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Investigation of 1 N -substituted pyrazole-3-carboxanilides as 15-lipoxygenase-1 (15-LOX-1) inhibitors demonstrated that the 1 N -substituent was not essential for activity or selectivity. Additional halogen substituents on the pyrazole ring, however, increased activity. Further development led to triazole-4-carboxanilides and 2-(3-pyrazolyl) benzoxazoles, which are potent and selective 15-LOX-1 inhibitors.