The invention provides a cephalosporins compound and a preparation method and use thereof. Propynyloxy, butynyloxy or furylmethoxy are introduced at 7Alpha-bit, and suitable 7Beta-bit and other substituted bit groups are selected to prepare the compound of which the antibacterial activity is obviously better than the current cephalosporins pharmaceuticals. The structural formula of the obtained compound is as shown in the formula (I). The obtained compound has excellent antibacterial activity, and has good effect to methicillin drug-resistant staphylococcus aureus especially, wherein the effect is multiple times better than the cephalosporins pharmaceuticals in the market. The preparation method for the cephalosporins compound has the characteristics of simple process and high efficiency. The environment-unfriendly chemical reagents are avoided to be used in the synthetic process, the experimental procedure operation is simple and convenient, and the preparation method is good for industrial large-scale production.