Synthesis of some new fluorine containing 1,3,4-oxadiazole derivatives as potential antibacterial and anticancer agents^§

1765-1769The synthesis of a number of 1,3,4-oxadiazole derivatives have been described. 2,4-Dichloro-5-fluorobenzoyl hydrazine 1 on reacting with aromatic acids in presence of phosphorus oxychloride affords 2,5-disubstituted- 1,3,4-oxadiazoles 2a-j. Aroyl hydrazine on reacting with carbon disulphide under basic condition gives oxadiazol-2-thione 3. Oxadiazol-2-thiones are regioselectively aminomethylated to give N-aminomethylated products 4a-c. Further, 3 undergoes regioselective alkylation on treating with alkyl/aroyl halides to give S-alkyl /aroyl products 5a-c. All the newly synthesized compounds have been screened for their anti bacterial activity. Most of them show promising anti bacterial activity. Also two out or nine compounds show anticancer activity in the primary anticancer assay