K. Raju

Design and synthesis of positional isomers of 1-alkyl-2-trifluoromethyl-5 or 6-substituted benzimidazoles and their antimicrobial activity

A series of novel positional isomers of 1-alkyl-2-trifluoromethyl benzimidazole derivatives 3a–j and 4a–j have been synthesized and screened for antibacterial activity against gram positive bacteria viz, Bacillus subtilis, Staphylococcus aureus and gram negative bacteria viz., Escherichia coli, Pseudomonas aeruginosa and antifungal activity against Candida albicans, Aspergillus niger, Rhizopus oryzae and Saccharomyces cerevisiae. Results indicate that compounds 3b, 4b were having promising antibacterial and antifungal activity.

Synthesis of novel optically pure α-amino acid functionalised-7-trifluoromethyl substituted quinolone derivatives and their antibacterial activity

Abstract7-Trifluoromethyl-4-hydroxy quinoline-3-carboxylic acid ethyl ester was prepared from 3-amino benzotrifluoride and EMME. The hydroxyquinoline was reacted with amino acids to furnish amino acid funtionalised quinolines (5, 6, 7). The compounds were alkylated by ethyl iodide followed by hydrolysis afforded the title compounds in good yields. They were screened for their antibacterial activity for in vitro against Gram +ve and Gram −ve bacterial strains and found 11e and 11b as promising compounds.

Trace Level Determination of Mesityl Oxide and Diacetone Alcohol in Atazanavir Sulfate Drug Substance by a Gas Chromatography Method.

A capillary gas chromatography method with a short run time, using a flame ionization detector, has been developed for the quantitative determination of trace level analysis of mesityl oxide and diacetone alcohol in the atazanavir sulfate drug substance. The chromatographic method was achieved on a fused silica capillary column coated with 5% diphenyl and 95% dimethyl polysiloxane stationary phase (Rtx-5, 30 m x 0.53 mm x 5.0 µm). The run time was 20 min employing programmed temperature with a split mode (1:5) and was validated for specificity, sensitivity, precision, linearity, and accuracy. The detection and quantitation limits obtained for mesityl oxide and diacetone alcohol were 5 µg/g and 10 µg/g, respectively, for both of the analytes. The method was found to be linear in the range between 10 µg/g and 150 µg/g with a correlation coefficient greater than 0.999, and the average recoveries obtained in atazanavir sulfate were between 102.0% and 103.7%, respectively, for mesityl oxide and diacetone alcohol. The developed method was found to be robust and rugged. The detailed experimental results are discussed in this research paper.