Synthesis, in silico studies and antibacterial assessment of α-amino phosphonates derivatives

The widespread of multi-resistant strains due to the lack of specific treatment and the propagation of infectious diseases requires all resources to remedy this scourge. This study is therefore aimed to assess the antibacterial activity of four synthetic α-Aminophosphonate 4(a-d). Methods: Firstly, α-Aminophosphonate has been synthesized and characterized, then molecular docking of these compounds 4(a-d) into the active binding site of Escherichia coli MurB enzyme (PDB Id: 1MBT) was performed to gain a comprehensive understanding of their biological activity. These compounds have been subjected to in vitro antibacterial screening against three multi-resistant strains E. coli, S. aureus, and L. monocytogenes. These compounds showed crucial antibacterial behavior against all studied strains. Thus, their docking estimation supported the in vitro results and showed that the 4c derivative has considerable binding energy towards the active site of Escherichia coli MurB. These findings provide critical information for the exploration of α-amino phosphonates as novel antibacterial agents.

A Green Protocol for the Synthesis of α-Amino Phosphonates Catalyzed by Orange Peel Powder

A simple and green protocol has been developed for the synthesis of α-aminophosphonates from different substituted aromatic aldehydes, aniline and dimethyl phosphite in the presence of orange peel powder (OPP) as a natural catalyst under reflux conditions. The main advantages of this method are the high yield of product, simple workup procedure, short reaction time and easily available catalyst.

Enantioselective Hydrophosphonylation of N-Boc Imines using Chiral Guanidine–Thiourea Catalysts

The enantioselective hydrophosphonylation of N-Boc imines was investigated using a new family of pseudo-symmetric guanidine–thiourea catalysts, providing -amino phosphonates in moderate to high yields with good enantioselectivity. The catalyst was...

Energy-, time-, and labor-saving synthesis of α-ketiminophosphonates: Machine-learning-assisted simultaneous multiparameter screening for electrochemical oxidation

A Highly efficient synthesis of α-ketiminophosphonates has been established for the electrochemical oxidation of α-amino phosphonates with the utilization of machine-learning-assisted simultaneous multiparameter screening. After brief experimental screening, the Bayesian...