Neuraminidase (NA) is the major surface glycoprotein of the influenza virus. It has been considered a suitable target for designing agents against influenza viruses. Rational drug design of NA inhibitors is now in the clinic and is effective for the treatment of influenza. Recently, research of structure-based NA inhibitors is becoming an interesting field, leading to a breakthrough in the control of influenza. Here we review a series of neuraminidase inhibitors and the recent progress in this field.