Author/Authors :
Hariri, Elham Department of Medicinal Chemistry, School of Pharmacy - Phytochemistry Research Center - Shahid Beheshti University of Medical Sciences , Tehrani, Mohammad Ebrahim Department of Medicinal Chemistry, School of Pharmacy - Phytochemistry Research Center - Shahid Beheshti University of Medical Sciences , Mashayekhi, Vida Department of Medicinal Chemistry, School of Pharmacy - Phytochemistry Research Center - Shahid Beheshti University of Medical Sciences , Kobarfard, Farzad Department of Medicinal Chemistry, School of Pharmacy - Phytochemistry Research Center - Shahid Beheshti University of Medical Sciences , Mahboubi, Arash Department of Pharmaceutics - School of Pharmacy - Shahid Beheshti University of Medical Sciences , Rahmani, Parisa Department of Pharmaceutics - School of Pharmacy - Shahid Beheshti University of Medical Sciences , Babaeian, Mohammad Department of Pharmaceutics - School of Pharmacy - Shahid Beheshti University of Medical Sciences , Fathi, Mohammad Department of Anestesiology - Shahid Modarres Hospital - Shahid Beheshti University of Medical Sciences, Tehran
Abstract :
A series of hydroxyl semicarbazone derivatives of substituted diaryl ketones and acetophenones
were synthesized and their structures were confirmed by analytical and spectroscopic methods
including elemental analysis, infrared and nuclear magnetic resonance spectroscopy. The
derivatives were prepared by a condensation reaction between N-hydroxy semicarbazide and
substituted diaryl ketones or acetophenones leading to the desired hydroxysemicarbazones with
excellent purity. The synthesized hydrazones were then evaluated for their inhibitory activity
against bacterial strains including S. aureus, E. Coli, P. aeruginosa, K. pneumonia and M. luteus.
Among the tested derivatives, compounds 2, 6 and 7 exhibited the highest bioactivity. Analysis
of the activity data suggests that hydrophilicity is an important factor for the bioactivity of
compounds 2 and 6 and also their selectivity over the gram-negative bacteria
Keywords :
N-hydroxy semicarbazone , Antibacterial , Broth microdilution assay , Ketones; Hydrophilicity