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 an...

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Published inJournal of enzyme inhibition and medicinal chemistry Vol. 24; no. 2; p. 566
Main Authors Gholivand, Khodayar, Abdollahi, Mohammad, Mojahed, Fresia, Alizadehgan, Ahlam Madani, Dehghan, Gholamreza
Format Journal Article
LanguageEnglish
Published England 01.04.2009
Subjects
Acetylcholinesterase - metabolism
Amides - chemistry
Amides - pharmacology
Animals
Butyrylcholinesterase - metabolism
Cattle
Cholinesterase Inhibitors - chemistry
Cholinesterase Inhibitors - pharmacology
Humans
Inhibitory Concentration 50
Kinetics
Mice
Mice, Inbred Strains
Phosphoric Acids - chemistry
Phosphoric Acids - pharmacology
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Summary: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.
ISSN:1475-6374
DOI:10.1080/14756360802316971