氯萘磺酰胺类化合物的合成与蛋白激酶C免疫调节作用

Studies on Protein Kinase C Immune Modulation Agents and Synthesis of 5-Chloro-1-Naphthalenesulfonamides

为了研究蛋白激酶Ｃ（ＰＫＣ）抑制剂及激活剂对巨噬细胞释放肿瘤坏死因子（ＴＮＦ）的影响，作者设计并合成了十八个５－氯－１－萘磺酰胺类化合物，经初步药理试验表明，本类化合物中的抑制剂均能显著抑制ＴＮＦ释放，而激活剂单独应用时不能引起ＴＮＦ释放，但可增强内毒素引起的ＴＮＦ释放。

To study the effects of protein kinase C(PKC)inhibitors and activators on therelease of tumor necrosis factor(TNF)from macrophages,eighteen analogs of 5-chloro-1-naphthalenesulfonamide were synthesized.Preliminary pharmacological results showed that all PKC inhibitors could significently inhibit the release of TNF whereas activators couldn't directly induce the release of TNF but could enhance the release of endotoxin-induced TNF.