The invention provides macrolide derivatives and application thereof. The general molecular formula of the macrolide derivatives is as shown in the description, wherein R1 is selected from hydrogen or a hydroxyl group or a halogen or a C1-C6 alkyl group or a C1-C4 alkoxy group or a C1-C6 alkenyl group or (CH2)m(C6-C10 aryl group) or (CH2)m(C5-C10 ceteroary) or a C2-C10 alkynyl group, R2 and R3 are each selected from hydrogen or a hydroxyl group or a halogen or a C1-C6 alkyl group or a C1-C6 alkenyl group or (CH2)m(C6-C10 aryl group) or (CH2)m(C5-C10 ceteroary) or a C2-C10 alkynyl group or a C1-C4 alkoxy group or a pyranose group, the pyranose group is unsubstituted or substituted with one or more of the following groups of hydrogen, halogen, a C1-C6 alkyl group, a C1-C4 alkoxy group, a C1-C4 alkyl acyl group and a C1-C4 alkyl acyloxy group, and each m is an independent integer ranging from 0 to 4. The compounds can be used for preparing drugs which have the function of promoting alimentary motility and are low in antibiotic activity and small in side effect.