The continued emergence of drug-resistance to existing antibacterial agents represents
a severe and ongoing public health concern, which demands the discovery of new antibiotics.
However the number of novel classes of antibacterial drugs launched in the clinic
has been remarkably slow since the 1960s, and it is urgent to develop novel antibacterial
agents to fight against drug-resistant bacterial pathogens. Peptidoglycan is a component of
the bacterial cell wall, which consists of a repeated N-acetylmuramic acid (MurNAc) and Nacetylglucosamine
(GluNAc) polymer cross-linked with polypeptides, and is a good target for antibacterial
drug discovery. Among enzymes responsible for its biosynthesis, phospho-MurNAc-pentapeptide translocase
(MraY) is a novel and promising target. Many nucleoside natural products, which strongly inhibit MraY, have
been found in nature. This review will summarize the synthesis and biological properties of selected MraY
inhibitory nucleoside natural products and their analogues synthesized in our laboratory and by others.
Keywords: Nucleoside antibiotics, MraY, natural products, antibacterial, drug-resistance, total synthesis.
Rights & PermissionsPrintExport