Abstract：
The prevention or control of bacterial infections requires continuous search for novel approaches among which bacterial quorum sensing inhibition is considered as a complementary antibacterial strategy. Quorum sensing, used by many different bacteria, functions through a cell-to-cell communication mechanism relying on chemical signals, referred to as autoinducers, such as N-acyl homoserine lactones (AHLs) which are the most common chemical signals in this system. Designing analogs of these autoinducers is one of the possible ways to interfere with quorum sensing. Since bioisosteres are powerful tools in medicinal chemistry, targeting analogs of AHLs or other signal molecules and mimics of known QS modulators built on amide bond bioisosteres is a relevant strategy in molecular design and synthetic routes. This review highlights the application of amide bond bioisosteric replacement in the design and synthesis of novel quorum sensing inhibitors.
摘要：
预防或控制细菌感染需要不断寻找新的方法，其中细菌群体感应抑制被认为是一种补充的抗菌策略。法定人数感应,被许多不同的细菌使用，通过依赖于化学信号的细胞间通讯机制发挥作用，称为自动诱导器，例如N-酰基高丝氨酸内酯(AHL),其是该系统中最常见的化学信号。设计这些自诱导物的类似物是干扰群体感应的可能方式之一。由于生物均衡是药物化学中的强大工具，AHL或其他信号分子的靶向类似物和基于酰胺键生物等排体的已知QS调节剂的模拟物是分子设计和合成途径中的相关策略。本文综述了酰胺键生物等排置换在设计和合成新型群体感应抑制剂中的应用。
