Fused pyrimidine derivativesFused pyrimidine derivatives R 0515 A Novel Orally Active Inhibitor of HLE. -The synthesis of compound (IX), a potential orally active HLE inhibitor for the treatment of inflammatory bronchopulmonary diseases such as COPD and chronic bronchitis, is presented. Ex vivo experiments in mice and the in vivo acute HLE induced mouse lung haemorrhage model demonstrate the remarkable oral activity of this new substance. -(VARGA*, M.; KAPUI, Z.; BATORI, S.; NAGY, L. T.; VASVARI-DEBRECZY, L.; MIKUS, E.; URBAN-SZABO, K.; ARANYI, P.; Eur. J. Med. Chem. 38 (2003) 4, 421-425; Discovery Res., CHINOIN Co. Ltd., H-1045 Budapest, Hung.; Eng.) -H. Haber 37-130
The antiostheophorotic agent ipriflavone [7-(1-methyl-ethoxy)-3-phenyl-4H-1-benzopyran-4-one, C18H16O3] is an important member of the isoflavone family. The structure of the molecule is dominated by the dihedral angle (50 degrees) between the planes of the phenyl and benzo-pyran moieties. A structural comparison with other related published structures is represented.
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