167758-80-7Relevant academic research and scientific papers
Novel imidazole compounds as a new series of potent, orally active inhibitors of 5-lipoxygenase
Mano, Takashi,Stevens, Rodney W.,Ando, Kazuo,Nakao, Kazunari,Okumura, Yoshiyuki,Sakakibara, Minoru,Okumura, Takako,Tamura, Tetsuya,Miyamoto, Kimitaka
, p. 3879 - 3887 (2007/10/03)
Replacement of the dihydroquinolinone pharmacophore of Zeneca's ZD2138 by ionizable imidazolylphenyl moiety has lead to the discovery of a novel series of potent and orally active 5-lipoxygenase (5-LO) inhibitors. The synthesis and structure-activity relationship (SAR) of this series of compounds are described herein.
Imidazole lipoxygenase inhibitors
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, (2008/06/13)
Certain novel imidazole derivatives having the ability to inhibit the lipoxygenase enzyme and having formula (I), wherein Y is hydrogen, C1 -C8 alkyl, halosubstituted C1 -C4 alkyl, phenyl, substituted phenyl, C7 -C14 phenylalkyl, C7 -C14 (substituted phenyl)alkyl, pyridyl, substituted pyridyl, C6 -C13 pyridylalkyl or C6 -C13 (substituted pyridyl)alkyl, wherein each substituent is independently halo, nitro, cyano, C1 -C4 alkyl, C1 -C4 alkoxy, halosubstituted C1 -C4 alkyl, halosubstituted C1 -C4 alkoxy, NR4 R5, CO2 R4 or CONR4 R5, wherein R4 and R5 are each, independently, hydrogen or C1 -C6 alkyl; Ar1 and Ar2 are each, independently, phenylene, mono-substituted phenylene or di-substituted phenylene, wherein the substituents are, independently, halo, C1 -C4 alkyl, C1 -C4 alkoxy, halo-substituted C1 -C4 alkyl or halo-substituted C1 -C4 alkoxy; X and X1 are each, independently, O, S, SO or SO2 ; R' is hydrogen or C1 -C4 alkyl; and R2 and R3 are each, independently, methylene, ethylene or propylene. These compounds are useful for the treatment of disease states such as bronchial asthma, skin disorders and arthritis in mammals, and as the active ingredient in pharmaceutical compositions for treating such conditions.
