SYNTHESIS, CHARACTERIZATION, AND IN-SILICO ADMET STUDIES OF SOME NEW PHENYLHYDRAZONE DERIVATIVES AS POTENT FOR ANTIMICROBIAL ACTIVITIES

ABSTRACT

Antimicrobial chemotherapeutic failure as a result of pathogenic resistance stain is great concern across the globe, there is need to search for an effective antimicrobial agent from synthetic sources to overcome emergent of microbial resistant in clinical practice. The phenylhydrazone derivatives were scientifically found to have wide application in area of drug discovery due to their anticancer, anti-tubercular, anti-bacterial and anti-fungal activities.

Five (5) novel (E)-Substituted-N-(phenylhydrazones) derivatives’ were obtained by condensation reaction between substituted acetophenone and substituted phenyl hydrazine through one step reaction, here are the five compounds, HS1 (E)-1-(1-(4-bromophenyl)ethylidene)-2-(2,4-dinitrophenyl)hydrazine),HS2 (E)-1-(1-(4-bromophenyl)ethylidene)-2-(4-nitrophenyl)hydrazine), HS3(E)-1-(4-nitrophenyl)-2-(1-(3-nitrophenyl)ethylidene)hydrazine), HS4 (E)-1-(2,4-dinitrophenyl)-2-(1-(3-nitrophenyl)ethylidene)hydrazine), and HS5 (E)-1-(1-(3-nitrophenyl)ethylidene)-2-phenylhydrazine) and their structural elucidation were established on the basis of FTIR, 1D and 2D NMR spectra and the Insilco prediction of physicochemical properties found within the Lipinski's rule of five and the newly synthesized compounds were subjected to antimicrobial assessment for an in-vitro test evaluation using inhibition zone technique, MIC, MBC and MFC.

Abbreviations:

• MIC: Minimal inhibitory concentration, ZOI; Zone of inhibition, MBC; Minimum Bactericidal concentration, MFC; Minimum Fungicidal concentration, FTIR; Fourier transform infrared, NMR; nuclear magnetic resonance, 1D; one-dimensional, 2D; two dimensional and HS1-5: synthetic hydrazone (symbolic code number)