3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1.

Basic Information

ID: ALA3603736

Journal: Bioorg Med Chem Lett

Title: 3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1.

Authors: Pelcman B, Sanin A, Nilsson P, No K, Schaal W, Öhrman S, Krog-Jensen C, Forsell P, Hallberg A, Larhed M, Boesen T, Kromann H, Vogensen SB, Groth T, Claesson HE.

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.

CiteXplore: 26037322

DOI: 10.1016/j.bmcl.2015.05.004

Patent ID: