title: N-Substituted pyrazole-3-carboxamides as inhibitors of human 15-lipoxygenase.
abstract: High-throughput screening was used to find selective inhibitors of human 15-lipoxygenase-1 (15-LOX-1). One hit, a 1-benzoyl substituted pyrazole-3-carboxanilide (1a), was used as a starting point in a program to develop potent and selective 15-LOX-1 inhibitors.
authors.affiliation: Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden. Electronic address: benjamin.pelcman@orgfarm.uu.se.
authors.forename: Benjamin
authors.initials: B
authors.lastname: Pelcman
authors.affiliation: Biolipox AB, Berzelius väg 3, SE-171 65 Solna, Sweden.
authors.forename: Andrei
authors.initials: A
authors.lastname: Sanin
authors.affiliation: Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden; Biolipox AB, Berzelius väg 3, SE-171 65 Solna, Sweden.
authors.forename: Peter
authors.initials: P
authors.lastname: Nilsson
authors.affiliation: Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden; Biolipox AB, Berzelius väg 3, SE-171 65 Solna, Sweden.
authors.forename: Wesley
authors.initials: W
authors.lastname: Schaal
authors.affiliation: Biolipox AB, Berzelius väg 3, SE-171 65 Solna, Sweden.
authors.forename: Kristofer
authors.initials: K
authors.lastname: Olofsson
authors.affiliation: Biolipox AB, Berzelius väg 3, SE-171 65 Solna, Sweden.
authors.forename: Christian
authors.initials: C
authors.lastname: Krog-Jensen
authors.affiliation: Biolipox AB, Berzelius väg 3, SE-171 65 Solna, Sweden.
authors.forename: Pontus
authors.initials: P
authors.lastname: Forsell
authors.affiliation: Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden.
authors.forename: Anders
authors.initials: A
authors.lastname: Hallberg
authors.affiliation: Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden.
authors.forename: Mats
authors.initials: M
authors.lastname: Larhed
authors.affiliation: MedChem ApS, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
authors.forename: Thomas
authors.initials: T
authors.lastname: Boesen
authors.affiliation: MedChem ApS, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
authors.forename: Hasse
authors.initials: H
authors.lastname: Kromann
authors.affiliation: Biolipox AB, Berzelius väg 3, SE-171 65 Solna, Sweden; Department of Medicine, Building A3:02, Karolinska University Hospital Solna and Karolinska Institutet, SE-171 76 Stockholm, Sweden.
authors.forename: Hans-Erik
authors.initials: HE
authors.lastname: Claesson
mesh_terms: D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D001093:Arachidonate 15-Lipoxygenase / Q000378:metabolism*; D006801:Humans; D016859:Lipoxygenase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000577:Amides; D016859:Lipoxygenase Inhibitors; D011720:Pyrazoles; C031280:pyrazole; D001093:Arachidonate 15-Lipoxygenase
keywords: 15-Lipoxygenase; Arachidonic acid; Inhibitors; Pyrazole