Acetylcholinesterase/Butyrylcholinesterase inhibition activity of some new carbacylamidophosphate deriviatives

Abstract

Eight newly synthesized carbacylamidophosphates with the general formula RC(O)NHP(O)Cl 2 with RvpClZC 6 H 4 1a, pBrZC 6 H 4 2a, C 6 H 5 3a, and pMeZC 6 H 4 4a and RC(O)NHP(O)(NC 4 H 8 O) 2 RvpClZC 6 H 4 1b, pBrZC 6 H 4 2b, C 6 H 5 3b, pMeZC 6 H 4 4b, were selected to compare the inhibition kinetic parameters, IC 50 , K i , k p and K D , 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.

A preliminary investigation of anticholinesterase activity of some Iranian medicinal plants commonly used in traditional medicine

“…The finding of this study shows that the four most active herbal extracts contained not only nitorgenic compound such as alkaloid but also these extracts also contain rich components of saponin, flavonoid, and essential oils [29-34]. The new area of interest in research involves both AChE inhibitors and BuChE inhibitors after recognition of BuChE activity in hippocampus of patients with AD [33,42,43]. Recent studies have work on dual inhibitors of AChE and BuChE [42,43].…”

“…The new area of interest in research involves both AChE inhibitors and BuChE inhibitors after recognition of BuChE activity in hippocampus of patients with AD [33,42,43]. Recent studies have work on dual inhibitors of AChE and BuChE [42,43]. In these studies synthesized chemical compounds have shown promising inhibitory effect on both AChE and BuChE [42-44].…”

Antibacterial activities of novel nanocomposite biofilms of chitosan/phosphoramide/Ag NPs

“…Recently, the phosphoramides chemistry has become very attractive owing to the various important applications of these molecules like anticancer prodrug compounds . Moreover, these derivatives are effective inhibitors for the ureas , acetylcholinesterase and butyrylcholinesterase enzymes. The biocidal activity of phosphoramides in agriculture is well known so that they are applied as pesticides and insecticides .…”

Phosphoramides: Synthesis, Spectroscopy, and X‐ray Crystallography

“…The highly enantioselective vinylogous addition of 2‐trimethylsilyloxyfuran to aldehydes was performed using chiral phosphoramides as Lewis bases . These types of compounds are also effective inhibitors for ureas , acetylcholinesterase , and butyrylcholinesterase enzymes. The biocidal activity of phosphoramides are well known so that they are applied as pesticides and insecticides in agriculture .…”