SYNTHESIS OF NEW TETRAZOLYL HYDROXYETHYL ACETAMIDES AS ANTI BACTERIAL AND ANTIPROTOZOAL AGENTS

2014 
Present investigation describes about the synthesis of some novel tetrazolyl hydroxyacetamides. These compounds were designed, based on the structure of etanidazole, an imidazole containing antiprotozoal drug and its radio protective activity is under clinical trials. Some new N-(2-hydroxyethyl)-2-(5-phenyl-1H-tetrazol-1-yl) acetamides (5a - 5h) were synthesized by 1, 3-dipolar cycloaddition of arylnitriles with sodium azide followed by reaction with ethyl chloroactetate and ethanolamine. The structures of the newly synthesized compounds were confirmed on the basis of physical, proton NMR, mass and IR spectral data. All the synthesized compounds were screened for in vitro antibacterial and anti protozoal activities and the results of some of the derivatives exhibited promising activities. The MIC values of the compounds 5b, 5e and 5h showed significant activity at a concentration of 1.56 and 12.5 µg/mL. Highest antiamoebic activity was observed with compounds 5a and 5h possessing
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