The invention discloses an N-aryl dithiopyrrolidone-pyrone heterozygous derivative as well as a preparation method and application thereof, and provides derivatives of which structural formulas are asshown in formulas (I) and (II) which are shown in the description. In the formulas, Ar is selected from C6 to C10 aryl or heterocyclic rings containing 1 to 3 heteroatoms which are respectively and independently selected from N, O or S, X is selected from one of NH, NCH3 and O, and n is independently selected from 2, 3, 4, 5, 6 and 7. During preparation, different N-aryl dithiopyrrolidone compounds are selected as raw materials to hybridize with a pyrone carboxylic acid derivative through acylation reaction, so that a target derivative is obtained. The prepared derivative, pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof is a bacteria RNA (Ribonucleic Acid) polymerase inhibitor and is used for development of antibacterial agents.