1322881-55-9Relevant articles and documents
Ultrasound-assisted one-pot synthesis of α-oxycarbanilinophosphonates via a three-component condensation of an aldehyde, diethyl phosphite and an isocyanate under solvent-free conditions
Kaboudin, Babak,Fallahi, Maryam
, p. 4346 - 4348 (2011)
An efficient one-pot method has been developed for the synthesis of α-oxycarbanilinophosphonates via a one-pot reaction of an aldehyde with diethyl phosphite in the presence of magnesium oxide followed by reaction with an isocyanate under solvent-free conditions using ultrasonic irradiation. This method is simple, rapid and good yielding.
Synthesis of α-oxycarbanilinophosphonates and their anticholinesterase activities: The most potent derivative is bound to the peripheral site of acetylcholinesterase
Kaboudin, Babak,Emadi, Saeed,Faghihi, Mohammad Reza,Fallahi, Maryam,Sheikh-Hasani, Vahid
, p. 576 - 582 (2015/02/19)
A novel method has been developed for the synthesis of α-oxycarbanilino phosphonates through a reaction of α-hydroxyphosphonates with isocyanate under microwave irradiation. The synthesized compounds were evaluated for their acetylcholinesterase (AChE) inhibition potency through IC50determination. Molecular modelling studies suggest that the most potent inhibitor (compound 4h, IC50 = 6.36 μM) is bound to the peripheral site of AChE, which suggests that it decreases the catalytic activity not through binding to the active site but through blocking the entrance of the active site gorge. This puts forward the potential of compound 4h and its derivatives to be used in the design of dual inhibitors: inhibition of the catalytic activity of AChE and of amyloid β aggregation.
Synthesis of α-oxycarbanilinophosphonates and their anticholinesterase activities: the most potent derivative is bound to the peripheral site of acetylcholinesterase
Kaboudin, Babak,Emadi, Saeed,Faghihi, Mohammad Reza,Fallahi, Maryam,Sheikh-Hasani, Vahid
, p. 576 - 582 (2013/05/08)
A novel method has been developed for the synthesis of α- oxycarbanilino phosphonates through a reaction of α-hydroxyphosphonates with isocyanate under microwave irradiation. The synthesized compounds were evaluated for their acetylcholinesterase (AChE) inhibition potency through IC50determination. Molecular modelling studies suggest that the most potent inhibitor (compound 4h, IC50 = 6.36 M) is bound to the peripheral site of AChE, which suggests that it decreases the catalytic activity not through binding to the active site but through blocking the entrance of the active site gorge. This puts forward the potential of compound 4h and its derivatives to be used in the design of dual inhibitors: inhibition of the catalytic activity of AChE and of amyloid β aggregation.