Open AccessSynthesis, characterization and antimicrobial activity of novel tetrazoles clubbed with pyrimidine
Author(s) -
N.D. Bhoge,
Baban K. Magare,
Popat Mohite
Publication year - 2021
Publication title -
journal of pharmaceutical and biological sciences
Language(s) - English
Resource type - Journals
ISSN - 2320-1924
DOI - 10.18231/j.jpbs.2021.016
Subject(s) - chemistry , tetrazole , thiourea , yield (engineering) , proton nmr , aryl , pyrimidine , antimicrobial , acetic anhydride , antibacterial activity , organic chemistry , medicinal chemistry , nuclear chemistry , bacteria , stereochemistry , catalysis , alkyl , materials science , biology , metallurgy , genetics
An attempt was made to synthesize pyrimidine tetrazole derivatives of pharmaceutical interest by oxidative cyclization of chalcones with adequate yield and purity, prompted by the diversity of their wider usage and the fact that they are an integral part of genetic content. The present work involves the reaction of 5-(2,6-dimethylphenyl)-1H-tetrazole with acetic anhydride to yield 1-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl] ethanone (1) and which then treated with different aromatic aldehydes in presence of alkaline medium to chalcones (2a-f). Reaction of chalcones (2a-f) with urea and thiourea to produce 5-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl]-4-(substituted aryl ) pyrimidin-2-ol (3a-f) and 5-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl]-4-(substituted aryl) pyrimidin-2-thiol (4a-f) respectively. All compounds were characterized by infrared spectroscopy (IR), H nuclear magnetic resonance (NMR), and mass spectrometry (MS) to prove the structure and assessed in vitro for their efficacy as antibacterial and antifungal activity against four bacteria. The compounds 3c, 3d and 3f and compounds 4c, 4d and 4f possess very good activity against and E. coli and the compounds 3e, 3c and 3a and compounds 4e,4b and 4c possess very good activity against fungi and .