Tian Tian, Weng Xiao-Cheng, Song Yang, Zhang Li-Xia, Zhou Xiang, Wang Yi
College of Chemistry and Molecular Sciences, Wuhan University, Hubei, Wuhan 430072, PR China.
Chem Biodivers. 2007 May;4(5):947-54. doi: 10.1002/cbdv.200790084.
A series of biphenol-derived quaternary ammonium salts, originally developed as DNA-cross-linking agents, and carrying either two (i.e., 1) or four (i.e., 2) net positive charges, were investigated for their in vitro DNA-transcription- and acetylcholinesterase (AChE)-inhibitory activities. The effects of charge and type of linker between the two phenolic residues were systematically investigated. Several compounds showed good activities in both tests, which makes them potential lead candidates for drug design.
一系列最初作为DNA交联剂开发的双酚衍生季铵盐，带有两个（即1）或四个（即2）净正电荷，对其体外DNA转录抑制活性和乙酰胆碱酯酶（AChE）抑制活性进行了研究。系统研究了两个酚羟基之间的电荷和连接基类型的影响。几种化合物在这两种测试中均表现出良好的活性，这使其成为药物设计潜在的先导候选物。
