The Synthesis and Evaluation of Amidoximes as Cytotoxic Agents on Model Bacterial E. coli Strains

• Published in: Materials Vol. 14; no. 24; p. 7577
• Main Authors: Samsonowicz-Górski, Jan, Kowalczyk, Paweł, Koszelewski, Dominik, Brodzka, Anna, Szymczak, Mateusz, Kramkowski, Karol, Ostaszewski, Ryszard
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 09-12-2021; MDPI
• Subjects: Acylation; Alkylation; amidoximes; Antibiotics; Antiinfectives and antibacterials; Bacteria; Biological activity; Boc-derived amidines; Boc-protected amidoximes; Chemical compounds; Chemical reactions; Chromatography; Cytotoxicity; Diarrhea; DNA-N-glycosylase; E coli; Ethanol; Fpg protein-formamidopyrimidine; Gene expression; Infections; lipopolysaccharide (LPS); lipopolysaccharide (LPS); DNA-N-glycosylase; Boc-derived amidines; Fpg protein-formamidopyrimidine; amidoximes; Boc-protected amidoximes
• ISSN: 1996-1944; 1996-1944
• DOI: 10.3390/ma14247577

The biological research on newly synthesized amidoximes, Boc-protected amidoximes and Boc-derived amidines, obtained by a reduction of the parent amidoximes is reported, herein. Due to the presence of a free amino group in both amidines and amidoximes, these compounds can undergo various chemical reactions such as
-alkylation and
-acylation. One such reaction is Boc-protection, often used in organic synthesis to protect the amino and imino groups. Until now, Boc-protected amidoximes have not been tested for biological activity. Amidoxime derivatives were tested on bacterial
strains. Initial cellular studies tests and digestion with Fpg after the modification of bacterial DNA, suggest that these compounds may have greater potential as antibacterial agents compared to antibiotics such as ciprofloxacin (ci), bleomycin (b) and cloxacillin (cl). The described compounds are highly specific for pathogenic
strains on the basis of the model strains used and may be used in the future as new substitutes for commonly used antibiotics in clinical and hospital infections in the pandemic era.