Lucas R, Ubeda A, Payá M, Alves M, del Olmo E, López J L, San Feliciano A
Departmento de Farmacología, Univ. de Valencia, Burjassot, Spain.
Bioorg Med Chem Lett. 2000 Feb 7;10(3):285-8. doi: 10.1016/s0960-894x(99)00680-0.
We have synthesised some lipidic diamines and aminoalcohols and examined their behaviour as inhibitors of secretory and cytosolic PLA2. Some structure-activity relationships considerations have been deduced. Compound 14 was a potent and selective inhibitor of cPLA2 and compound 4 showed a dual inhibitory profile against both types of PLA2 while no cytotoxicity at 10 microM on human neutrophils or on murine macrophage line was observed for both.
我们合成了一些脂族二胺和氨基醇，并研究了它们作为分泌型和胞质型磷脂酶A2抑制剂的行为。已经推导出了一些构效关系方面的考虑因素。化合物14是一种有效的cPLA2选择性抑制剂，化合物4对两种类型的磷脂酶A2均表现出双重抑制作用，并且在10微摩尔浓度下对人中性粒细胞或小鼠巨噬细胞系均未观察到细胞毒性。
