SYNTHESIS OF NEW TETRAZOLYL HYDROXYETHYL ACETAMIDES AS ANTI BACTERIAL AND ANTIPROTOZOAL AGENTS
Anitha Bhukya, Naresh K*, Madhava Reddy B, Harinadha Babu V
ABSTRACT
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
electron withdrawing substituents on phenyl ring.
Keywords: Arylnitriles; Substituted tetrazoles; Tetrazolyl acetamides; Antiprotozoal; Antibacterial.
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