3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1
B Pelcman, A Sanin, P Nilsson, K No, W Schaal… - Bioorganic & medicinal …, 2015 - Elsevier
B Pelcman, A Sanin, P Nilsson, K No, W Schaal, S Öhrman, C Krog-Jensen, P Forsell…
Bioorganic & medicinal chemistry letters, 2015•ElsevierInvestigation 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.
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.
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.
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