Adiel Coca
Professor, Southern Connecticut State University USA
Title: Preparation and Antimicrobial Properties of Tetrazole Derivatives
Biography
Biography: Adiel Coca
Abstract
The tetrazole ring has been featured in several approved anti-hypertension drugs such as losartan, olmesartan, irbesartan, valsartan, candesartan and fimasartan. Tetrazole derivatives have also been used as lipophilic spacers, peptide chelating agents, and as cis-peptide bond mimics. Perhaps the most common application of the tetrazole ring is as a bioisotere for carboxylic acids due to similar acidity and planarity. The tetrazole ring is typically synthesized via the (3+2) cycloaddition of an organonitrile and sodium azide in aprotic polar solvents such as dimethylformamide. In this work, several tetrazole derivatives were synthesized in good yields using a rare-earth metal catalyst. Microwave radiation was used to heat the reactions which were done in an aqueous solvent mixture. The antimicrobial properties of the resulting tetrazole derivatives were determined against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. Some tetrazole derivatives showed a significant synergistic effect when used in combination with trimethoprim.