N-(4-Substituted Aryl) amino acids as potential antibacterial agents

Abstract

Abstract Resistance of bacteria to current antibiotic drugs and the reoccurrence of different ailments after several therapeutic protocols have continued to be a cause of concern. Arylated amino acids are vital synthons to many compounds, they serve as essential building blocks in the synthesis of nitrogen heterocycles with various biological activities. This research reports the synthesis of some N-aryl amino acids and evaluates their antibacterial activities. The N-aryl amino acids 3a-3j were obtained by reacting different 4-substituted fluorobenzene 1a-1d with different amino acids 2a-2g via a metal-free, base-induced aryl amination reaction of aryl halides. The antibacterial activities of the synthesised compounds were evaluated against eight bacterial strains (Four gram-positive: Bacillus subtilis (ATCC 6633), Streptococcus pneumonia (ATCC 33400), Staphylococcus aureus (ATCC 25923), Staphylococcus epidermidis (ATCC 14990) and four gram-negative: Enterobacter cloacae (ATCC 43560), Escherichia coli (ATCC 25922), Proteus mirabilis (ATCC 43071) and Klebsiella oxytoca (ATCC 13182) using the agar well diffusion method with streptomycin as a reference drug. The biological screening indicates the synthesised compounds 3a, 3e, and 3j have promising broad-spectrum antibacterial potential as the N-aryl amino acid displayed comparable to better activity with the standard drug against Streptococcus pneumonia, Escherichia coli, and Proteus mirabilis.