Synthesis and antibacterial activity of 3-(4-amino-5-methyl-s-triazol-3-sulfanyl)-1-phenyl-propan-1-one O-(5-substituted phenyl-1,3,4 oxadiazol-2-methyl)-oximes / 药学学报

ABSTRACT

<p><b>AIM</b>To study the synthetic method and antibacterial activity of amino-heterocyclic compounds coupled oxime-ether group.</p><p><b>METHODS</b>The treatment of 4-amino-3-methyl-5-mercapto-s-triazole (3) with beta-chlorophenyl-propanone to form amino-s-triazole sulfanylphenyl-propanone (4) sequentially followed by oximation with hydroxyl-amine to produce the oximes (5) and etherification with various oxadiazole chloromethanes (6a - j) to yield the title compounds (1a - j). The in vitro antibacterial activities of all newly synthesized compounds were tested against Gram positive bacteria and Gram negative bacteria with the standard 2-fold agar dilution method.</p><p><b>RESULTS</b>Twelve new compounds including two intermediates were synthesized and their structures were confirmed by IR, 1H NMR, MS and elemental analyses. The ten title compounds exhibited the potential antibacterial activities in vitro.</p><p><b>CONCLUSION</b>Theses compounds should be optimized.</p>