Acetylcholinesterase/butyrylcholinesterase inhibition activity of some new carbacylamidophosphate derivatives.
Eight newly synthesized carbacylamidophosphates with the general formula RC(O)NHP(O)Cl2 with R = pCl-C6H4 1a, pBr-C6H4 2a, C6H5 3a, and pMe-C6H4 4a and RC(O)NHP(O)(NC4H8O)2 R = pCl-C6H4 1b, pBr-C6H4 2b, C6H5 3b, pMe-C6H4 4b, were selected to compare the inhibition kinetic parameters, IC50, Ki, kp and KD, on human erythrocyte acetylcholinesterase (hAChE) and bovine serum butyrylcholinesterase (BuChE), Also, the in vivo inhibition potency of compound 2a, 2b and 3a, were studied. The data demonstrates that compound 2a and compound 2b are the potent sensitive as AChE and BuChE inhibitors respectively, and the inhibition of hAChE is about 10-fold greater than that of BuChE.
Gholivand
Khodayar
K
Department of Chemistry, Faculty of Science, Tarbiat Modares University, Tehran, Iran. gholi_kh@modares.ac.ir
Abdollahi
Mohammad
M
Mojahed
Fresia
F
Alizadehgan
Ahlam Madani
AM
Dehghan
Gholamreza
G
D000110:Acetylcholinesterase / Q000378:metabolism*; D000577:Amides / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D002091:Butyrylcholinesterase / Q000378:metabolism*; D002417:Cattle; D002800:Cholinesterase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D051379:Mice; D008815:Mice, Inbred Strains; D010756:Phosphoric Acids / Q000737:chemistry / Q000494:pharmacology
D000577:Amides; D002800:Cholinesterase Inhibitors; D010756:Phosphoric Acids; C011067:phosphoramidic acid; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase