Inhibition of neutrophil O2− production by unsymmetrical methylene derivatives of benzopyrans: their use as potential antiinflammatory agents
作者:Mauro Mazzei、Ramona Dondero、Enzo Sottofattori、Edon Melloni、Roberto Minafra
DOI:10.1016/s0223-5234(01)01279-x
日期:2001.12
Some unsymmetrical derivatives of benzopyrans 9 were synthesized and tested to verify their PKC inhibitory activity. For this purpose, the Mannich bases of 7-hydroxycoumarins 6 were treated with 2-(dialkylamino)benzopyran-4-ones or 3-(dialkylamino)naphtho[2,1-b]pyran-1-ones 8 in the presence of acetic or propionic anhydride, yielding compounds 9. Human neutrophils stimulated with either PMA and f-MLF
合成并测试了苯并吡喃9的一些不对称衍生物,以验证其对PKC的抑制活性。为此,在乙酸存在下,用2-(二烷基氨基)苯并吡喃-4-酮或3-(二烷基氨基)萘并[2,1-b]吡喃-1-酮8处理7-羟基香豆素6的曼尼希碱。用丙酸酐或丙酸酐产生化合物9。用PMA和f-MLF刺激的人类嗜中性粒细胞用作细胞模型。化合物9的效率建立在其减少活化的人类嗜中性粒细胞产生O(2)(-)的能力上。在色酮部分的7位带有乙酰氧基的化合物9d和9f似乎有效地抵消了中性粒细胞的活化。