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Pelcman B.,Uppsala University | Sanin A.,Biolipox AB | Nilsson P.,Uppsala University | Nilsson P.,Biolipox AB | And 11 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

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. © 2015 Elsevier Ltd. All rights reserved.


Pelcman B.,Uppsala University | Sanin A.,Biolipox AB | Nilsson P.,Uppsala University | Nilsson P.,Biolipox AB | And 14 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

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. © 2015 Elsevier Ltd. All rights reserved.

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