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Preparation, spectroscopic, and biological characterizations of novel α-aminophosphonates bearing paracetamol

Omar M Ali, Hamada H Amer, Eman-Abdeen, Omima H Khallaf.




Abstract

Background: α-Aminophosphonate derivatives have an important biological activity against bacteria, fungi, and anticancer activity.

Aims and Objectives: This study aims to study preparation, spectroscopic, and biological characterizations of novel α-aminophosphonates bearing paracetamol.

Materials and Methods: A series of α-aminophosphonate analogs and arylidene derivatives were synthesized, monitored by thin-layer chromatography, purified by chromatographic methods, and the structures were elucidated by spectroscopic methods such as H nuclear magnetic resonance. The synthesized compounds were tested for their antibacterial activity by hole well method against Escherichia coli (Gram-negative) and Staphylococcus aureus (Gram-positive), the antibacterial activity was evaluated based on inhibition zone size around dishes against Gram-positive.

Results: Compounds 7e, 8a, 7c, 8b, and 8g are showed different degree of inhibitory effect against S. aureus; on the other hand in Gram-negative, the compounds 7a, 7c, 7d, 7e, 8a, 8b, and 8g are showed different degree of inhibitory effect against E. coli. In this study, we concluded that the results showed that increasing the zone inhibition in compared with amoxicillin and tetracycline against E. coli and S. aureus. Most of the compounds tested against microbes showed a moderate to high effect while few compounds showed a low antimicrobial effect.

Conclusion: In this study, we recommended that α-aminophosphonate and arylidene derivatives used as antimicrobial agents.

Key words: Arylidene Derivatives; α-Aminophosphonates; Antimicrobial activity






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