Design, synthesis and biological evaluation of novel antipyrine based α-aminophosphonates as anti-Alzheimer and anti-inflammatory agent

Synthesis and Biological Studies of Novel Aminophosphonates and Their Metal Carbonyl Complexes (Fe, Ru)

“…Interestingly, the new ortho -substituted aminophosphonate 8a was found to be the most active of all tested compounds with an IC 50 value of 1.215 µM towards AChE. This result corroborates with our theoretical prediction, presented later, and is in good agreement with some recently reported activities of different aminophosphonates on the cholinergic system [ 43 , 44 , 45 ]. For example, a chromone-derived aminophosphonate acts as an acetylcholinesterase inhibitor with IC 50 = 0.103 µM.…”

“…This study has presented a novel approach to accessing some (aminomethyl)benzylphosphonates and their metallocarbonyl derivatives. Our findings are in good agreement with the results of other research teams on aminophosphonates [ 43 , 44 , 45 ]. They clearly indicate that the aminophosphonates provide a good basis for the development of an effective substance that inhibits the cholinergic system.…”

Enzymatic Synthesis of a Novel Coumarin Aminophosphonates: Antibacterial Effects and Oxidative Stress Modulation on Selected E. coli Strains

“…However, a majority of them are toxic, expensive, and have to be used in stoichiometric amounts. Moreover, reported methods suffer from some drawbacks, such In the last decade, α-aminophosphonates were intensively studied as a significant group of compounds because of their high biological activity [19][20][21], which broadens their applicability in agricultural and medicinal chemistry. Organophosphorus compounds are known for their antimicrobial activity (alafosfalin); for example, dialkyl αaminophosphonates exhibit activity against pathogenic E. coli, S. aureus, Bacillus, or K. pneumonia strains (Figure 1) [22][23][24][25].…”

Synthesis, in silico ADMET prediction analysis, and pharmacological evaluation of sulfonamide derivatives tethered with pyrazole or pyridine as anti-diabetic and anti-Alzheimer's agents

“…In the last decade, organic and pharmaceutical researchers have especially focused on antipyrine derivatives which possess a broad spectrum of therapeutic and clinical applications. Moreover, there are some antipyrine-based commercially available drugs such as Famprofazone and Edaravone ( Sahoo et al, 2020 , Ebosie et al, 2021 , Mustafa et al, 2022 , Shaikh et al, 2023 ). In 2023, Al-Sanea and co-workers prepared an oxadiazolyl linked to antipyrine derivative I , which demonstrated anti-inflammatory activity and selective inhibitory activity against COX-2 enzymes ( Al-Sanea et al, 2023 ).…”