Abstract:
The drug resistance phenomenon in microbes is resulting in the ineffectiveness of available drugs to treat the
infections. Thus, there is a continued need to discover new molecules to combat the drug resistance phenomenon.
Norfloxacin is a fluoroquinolone antibiotic that is used for the treatment of urinary tract infections. In this research work,
norfloxacin is structurally modified by hybridizing with a range of substituted acetohydrazidic moieties through a
multistep reaction. The first step involves the coupling of norfloxacin 1 with methyl chloroacetate followed by the
treatment with hydrazine hydrate to result in corresponding acetohydrazide 3. A range of substituted benzaldehydes were
reacted with the acetohydrazide to form the targeted series of norfloxacin derivatives 4a-i. The final compounds were
screened for antimicrobial activity. Among the tested compounds, 4c, 4d, 4e and 4f displayed better antifungal activity
against F.avenaceum, while compound 4c and 4e were active against F. bubigeum.
