Østby O B, Gundersen L L, Rise F, Antonsen O, Fosnes K, Larsen V, Bast A, Custers I, Haenen G R
Department of Chemistry, University of Oslo, P.O. Box 1033, Blindern, N-0315 Oslo, Norway.
Arch Pharm (Weinheim). 2001 Jan;334(1):21-4. doi: 10.1002/1521-4184(200101)334:1<21::aid-ardp21>3.0.co;2-w.
5-Substituted pyrrolo[1,2-b]pyridazines have been prepared by cyclisation of pyridazine with diphenylcyclopropenone followed by further functionalisations in the pyrrolo[1,2-b]pyridazine 5-position. Several compound exhibit profound inhibition of lipid peroxidation in vitro. Lipid peroxidation of boiled rat liver microsomes was induced by ascorbic acid/FeSO4 and the peroxidation was determined by measuring the thiobarbituric acid reactive material.
5-取代的吡咯并[1,2 - b]哒嗪是通过哒嗪与二苯基环丙烯酮环化,然后在吡咯并[1,2 - b]哒嗪的5-位进行进一步官能化反应制备而成。几种化合物在体外对脂质过氧化表现出显著抑制作用。用抗坏血酸/硫酸亚铁诱导煮沸的大鼠肝微粒体发生脂质过氧化反应,并通过测量硫代巴比妥酸反应性物质来测定过氧化程度。