Master Hoshang E, Khan Shabana I, Poojari Krishna A
Department of Chemistry, St. Xavier's College, 5, Mumbai, India.
Bioorg Med Chem Lett. 2003 Apr 7;13(7):1249-51. doi: 10.1016/s0960-894x(03)00112-4.
An attempt was made to synthesize a series of non-cytotoxic low molecular weight meta-substituted aromatic ethers (2-4, 5-7) and some of their bioisosteres (14-16) and to evaluate their activity on the activation of human complement (classical pathway) and their intrinsic hemolytic activity. The in vitro assay results of the inhibition of complement-mediated hemolysis by these analogues indicate that the aldehydic meta substituted aromatic ethers show inhibitory potency, while carboxylic acid meta substituted aromatic ethers show hemolytic activity. Some of the bioisosteres exhibit both inhibitory as well as hemolytic property.
人们尝试合成一系列无细胞毒性的低分子量间位取代芳香醚（2 - 4、5 - 7）及其一些生物电子等排体（14 - 16），并评估它们对人补体激活（经典途径）的活性及其内在溶血活性。这些类似物对补体介导的溶血抑制作用的体外测定结果表明，醛基间位取代芳香醚具有抑制效力，而羧酸间位取代芳香醚具有溶血活性。一些生物电子等排体兼具抑制和溶血特性。
