Abstract:
The versatile basic structure of piperazine allows for the development and production of newer bioactive molecules that can be used to treat a wide range of diseases. Piperazine derivatives are unique and can easily be modified for the desired pharmacological activity. The two opposing nitrogen atoms in a six-membered piperazine ring offer a large polar surface area, relative structural rigidity, and more acceptors and donors of hydrogen bonds. These properties frequently result in greater water solubility, oral bioavailability, and ADME characteristics, as well as improved target affinity and specificity. Various synthetic protocols have been reported for piperazine and its derivatives. In this review, we focused on recently published synthetic protocols for the synthesis of the piperazine and its derivatives. The structure-activity relationship concerning different biological activities of various piperazine-containing drugs has also been highlighted to provide a good understanding to researchers for future research on piperazines.
摘要:
哌嗪的通用基本结构允许开发和生产可用于治疗多种疾病的新型生物活性分子。哌嗪衍生物是独特的并且可以容易地修饰以获得所需的药理活性。六元哌嗪环中的两个相对的氮原子提供了大的极性表面积,相对结构刚度,和更多的氢键受体和供体。这些特性通常会导致更大的水溶性,口服生物利用度,和ADME特性,以及改善的靶标亲和力和特异性。已经报道了哌嗪及其衍生物的各种合成方案。在这次审查中,我们专注于最近公布的哌嗪及其衍生物的合成方案。还强调了有关各种含哌嗪药物的不同生物活性的结构-活性关系,为研究人员对哌嗪的未来研究提供了很好的理解。