title: 3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1.
abstract: Investigation of 1N-substituted pyrazole-3-carboxanilides as 15-lipoxygenase-1 (15-LOX-1) inhibitors demonstrated that the 1N-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.
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: Biolipox AB, Berzelius väg 3, SE-171 65 Solna, Sweden.
authors.forename: Kiyo
authors.initials: K
authors.lastname: No
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: Sara
authors.initials: S
authors.lastname: Öhrman
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: MedChem ApS, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
authors.forename: Stine Byskov
authors.initials: SB
authors.lastname: Vogensen
authors.affiliation: MedChem ApS, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
authors.forename: Thomas
authors.initials: T
authors.lastname: Groth
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: D001093:Arachidonate 15-Lipoxygenase / Q000378:metabolism*; D001583:Benzoxazoles / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D016859:Lipoxygenase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D001583:Benzoxazoles; D016859:Lipoxygenase Inhibitors; D011720:Pyrazoles; D014230:Triazoles; C031280:pyrazole; D001093:Arachidonate 15-Lipoxygenase
keywords: 15-Lipoxygenase; Arachidonic acid; Benzoxazole; Inhibitors; Pyrazole; Triazole