Synthesis, characterisation and antibacterial evaluation of some novel 1-phenyl-1h-tetrazole-5-thiol derivatives

Abstract

The aim of the study is to synthesise and. Characterize — some novel, "tetrazole., -5-thiol” derivatives. Firstly, the “1-phenyl-1H7-tetrazole-5-thiol” (A1) has been., synthesised by the reaction of phenylisothiocyanate with NaN3 in water as a solvent. Secondly, the tetrazole-5-thiol derivatives (A2-A4) were synthesised by the alkylation reaction of the compound (A1) with chloroacetone, phenacyl bromide and chloromethyl acetate respectively. The resulted percentage yield was relatively high (92%, %95, %90 respectively). Compound (A5) was synthesised by the reaction of ethyl acetate tetrazole derivative (A4) with hydrazine. Moreover, the derivatives (A6-A11) were synthesised by the reaction of the (A5) with various substituted aromatic aldehydes. Moreover, compounds (A12-A13) have been synthesised by the cyclization reaction of compound A5 with acetylacetone and phenyl acetylacetone respectively. The produced compounds have been identified by IR, 13C-NMR and 1H-NMR Spectroscopy, and the quantities of various of the physical data (melting point, the shape of crystal and color). Finally, the compounds were examined for their biological activities alongside two kinds of bacteria (E. Coli and Staphylococcus aureus). Compounds A2, A4, A8, A11 and A13 showed the highest inhibition activity against E. Coli. Compounds A2, A9, A10and A13 showed the maximum activity against Staphylococcus aureus.