Synthesis, molecular properties and anthelmintic activity of some schiff bases of 1, 3, 4 thiadiazole derivatives
By Bijo Mathew, Shyam Sankar Vakketh and Shyam. Sasi. Kumar
Our research concentrates on the synthesis of some Schiff bases of 5-phenyl substituted, 2-amino 1, 3, 4 thiadiazole derivates. The synthesis involves reaction between various aryl carboxylic acids with thiosemicarbazide in presence of dehydrating agent like Conc. H2SO4 to form 5-phenyl substituted, 2-amino 1, 3, 4 thiadiazole derivates. These derivatives on further treatment with various aldehydes to form Schiff base. The structures of the compounds were confirmed by IR, 1HNMR and elemental analysis. The physicochemical properties involve determination of drug-like property of the synthesized compounds. It is based on the Lipinski’s rule of 5 and can be determined by using molinspiration cheminformatics software. All the synthesized compounds showed zero violation of Lipinski’s rule of five, which indicates good bioactivity and bioavailabilty.The anthelmintic activity of those compounds was investigated by method described in details by Kuppast and Nayak.Parameters under study were mean paralysis and mean lethal time in Pheretima posthuma. All the compounds having significant activity than standard drug except compounds 3b, 3c and 3d.
Key Words: Schiff base, 1,3,4 thiadiazole, Lipinski’s rule of five, molinspiration, cheminformatics, Pheretima posthum