Insignificant level of in vitro cytotoxicity, anti‑rotavirus, antibacterial, and antifungal activities of N‑alkylmaleamic acids

Abstract

By reacting maleic anhydride with amines, we synthesized the derivatives N‑ethyl,
N‑(2‑ethylamine), N‑piperidinyl, N‑phenyl, and N‑phenylhydrazinyl maleamic acids.
The purity of these products was initially verified by melting range and the presence of
only one spot observed by thin layer chromatography. The chemical structures of the
obtained N‑alkyl maleamic acids were confirmed through infrared (IR) and hydrogen
and carbon nuclear magnetic resonance (1
H and 13C NMR) spectrometry. Due to
the already proven pharmacological activity of maleimides, maleic anhydride and its
N‑alkyl maleamic acids were subjected to in vitro assays to observe antiviral (SA‑11
rotavirus), antibacterial (Escherichia coli, Staphylococcus aureus, and Bacillus cereus),
antifungal (Colletotrichum musae, Fusarium solani f. sp. phaseoli, Fusarium solani f. sp.
piperis Alb., and Penicillium sp.), and antiprotozoal (Trichomonas vaginalis, Giardia
lamblia, and Entamoeba histolytica) effects. To study the anti‑rotavirus properties, firstly
the 3‑(4,5‑dimethylthiazol‑2‑yl)‑2‑5‑diphenyltetrazolium bromide (MTT) method was
used to establish the median cytotoxicity concentration (CC50) of the compounds, using
MA‑104 cell line. Under the experimental conditions used, cytotoxic, anti‑rotavirus,
antibacterial, and antifungal properties were not observed for these compounds.