Twelve Pyridinyl-4,5-2H-isoxazole Heterocyclic derivatives were synthesized from 2-chloro-5-chloromethylpyridine and their structures were characterized by 1HNMR, 13CNMR, MS and IR. The antibacterial activities results indicated all of them exhibited potent activities against Staphylococcus aureus (ATCC25923), Streptococcus pneumonia (ATCC49619) and Enterococcus faecalis (ATCC29212). Among of them, compound 9f and 9l showed the best activities. All the target compounds displayed excellent anthelmintic activities and the effects of compound 9a-b and 9g-h were much better than albendazole. This work provided a preliminary basis for developing novel antibacterial and anthelmintic agents. The further study on optimizing activities and mechanism-of-action is under investigation.