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Design, synthesis, and antimicrobial evaluation of some nifuroxazide analogs against nosocomial infection
Author(s) -
Dwivedi Deepak K.,
Sahu Adarsh,
Dighade Sachin J.,
Agrawal Ram Kishore
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3891
Subject(s) - chemistry , antimicrobial , hydrazide , aspergillus niger , escherichia coli , sulfuric acid , nuclear chemistry , in vitro , carbon 13 nmr , antibacterial activity , staphylococcus aureus , organic chemistry , bacteria , biochemistry , genetics , biology , gene
Abstract A series of 10 p ‐substitutedbenzoylmethylene hydrazide derivatives 4a‐j were synthesized by protecting carboxylic group of 4‐hydroxybenzoic acid using methanol and sulfuric acid than reacting it with hydrazide to form 4‐hydroxybenzohydrazide followed by reacting with a variety of aldehydes and evaluated for their activity against nosocomial infection. All the synthesized compounds were characterized by Fourier‐transform infrared (FT‐IR), 1 H nuclear magnetic resonance (NMR), and mass spectral data. The in vitro antimicrobial potential of synthesized compounds was estimated against prominent strains of nosocomial pathogens ( Staphylococcus aureus , Escherichia coli , and Aspergillus niger ). The antimicrobial evaluation revealed compounds 4b , 4c , 4d , 4e , 4f , and 4j to be the most active compounds of the series with IC 50 value for antibacterial in the range 0.39 to 0.75 μM/mL. Furthermore, the in vitro cytotoxic potential of the compounds was appraised by hemolytic assay. The results showed that some of the synthesized compounds exhibited marked activity.