Target Information

Target General Infomation
Target ID
T99799
Former ID
TTDS00143
Target Name
Cholinesterase
Synonyms
Acylcholine acylhydrolase; BuChE; Butyrylcholine esterase; Butyrylcholinesterase; Choline esterase II; Pseudocholinesterase
Target Type
Successful
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Neurotoxicity drug-induced [ICD10: T36-T50]
Poison intoxication [ICD10: T36-T50]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Spasms; Pain [ICD9: 338,780; ICD10: R52, G89]
Toxicity [ICD10: T36-T50, T51-T65]
Function
Esterasewith broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
BioChemical Class
Carboxylic ester hydrolase
Target Validation
T99799
EC Number
EC 3.1.1.8
Drugs and Mode of Action
Drug(s) Hexafluronium bromide Drug Info Approved Spasms; Pain [537810], [551871]
MEPTAZINOL Drug Info Approved Pain [551871]
(-)-Phenserine Drug Info Phase 3 Alzheimer disease [532220]
JES-9501 Drug Info Phase 1 Alzheimer disease [525989]
Plasma derived human butyrylcholinesterase Drug Info Phase 1 Neurotoxicity drug-induced [521839]
Protexia Drug Info Phase 1 Alzheimer disease [522424]
Inhibitor (+/-)-huprineY hydrochloride Drug Info [528570]
(-)-DEBROMOFLUSTRAMINE B Drug Info [529633]
(-)-Phenethylcymserine Drug Info [551218]
(-)-Phenserine Drug Info [551218]
(-)-Tolserine Drug Info [551218]
(1'H-Phenothiazin-1'-yl)(piperidin-1-yl)methanone Drug Info [530749]
(10H-phenothiazin-10-yl)(m-tolyl)methanone Drug Info [528978]
(10H-phenothiazin-10-yl)(o-tolyl)methanone Drug Info [528978]
(10H-phenothiazin-10-yl)(p-tolyl)methanone Drug Info [528978]
(10H-phenothiazin-10-yl)(phenyl)methanone Drug Info [528978]
(1R)-MENTHYL HEXYL PHOSPHONATE GROUP Drug Info [551374]
(1S)-MENTHYL HEXYL PHOSPHONATE GROUP Drug Info [551374]
(24S)-ethylcholesta-7,9(11),22(E)-triene-3b-ol Drug Info [527846]
(3-bromophenyl)(10H-phenothiazin-10-yl)methanone Drug Info [528978]
(4-bromophenyl)(10H-phenothiazin-10-yl)methanone Drug Info [528978]
(4-nitrophenyl)(10H-phenothiazin-10-yl)methanone Drug Info [528978]
(RS)-tacrine(10)-hupyridone Drug Info [529473]
1,10-bis(pyridinium)-decane dibromide Drug Info [530696]
1,11-bis(pyridinium)-undecane dibromide Drug Info [530696]
1,2-bis(2,3-fluorophenyl)ethane-1,2-dione Drug Info [528766]
1,2-di(10H-phenothiazin-10-yl)ethane-1,2-dione Drug Info [528978]
1,2-Di(berberine-9-O-yl)ethane dibromide Drug Info [530920]
1,2-indanedione Drug Info [529103]
1,2-NAPHTHOQUINONE Drug Info [529103]
1,3-Di(berberine-9-O-yl)ethane dibromide Drug Info [530920]
1,4-Di(berberine-9-O-yl)ethane dibromide Drug Info [530920]
1,9-bis(pyridinium)-nonane dibromide Drug Info [530696]
1-(10H-phenothiazin-10-yl)-2-phenylbutan-1-one Drug Info [528978]
1-(10H-phenothiazin-10-yl)-2-phenylethanone Drug Info [528978]
1-(10H-phenothiazin-10-yl)-2-phenylpropan-1-one Drug Info [528978]
1-(10H-phenothiazin-10-yl)-3-phenylbutan-1-one Drug Info [528978]
1-(10H-phenothiazin-10-yl)-3-phenylpropan-1-one Drug Info [528978]
1-(10H-phenothiazin-10-yl)-4-phenylbutan-1-one Drug Info [528978]
1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione Drug Info [528749]
1-methyl-3-(phenylcarbamoyloxy)pyridinium bromide Drug Info [551218]
2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine Drug Info [528402]
2-(N-Morpholino)-Ethanesulfonic Acid Drug Info [551393]
2-biphenyl-4-yl-1-phenothiazin-10-yl-ethanone Drug Info [528978]
2-methoxyphenyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
2-Methyl-beta-carboline-2-ium iodide Drug Info [530824]
2-Propyl-beta-carboline-2-ium iodide Drug Info [530824]
24-ethyl-cholest-7-ene-3,5,6-triol Drug Info [527846]
24-ethylcholest-6-ene-3,5-diol Drug Info [527846]
3,4,5,6-Tetrachloro-[1,2]benzoquinone Drug Info [527510]
3-(2-Diethylamino-acetamino)-rutaecarpine Drug Info [530639]
3-(2-Diethylamino-propionamino)-rutaecarpine Drug Info [530639]
3-(2-N-Piperidyl-propionamino)-rutaecarpine Drug Info [530639]
3-(2-N-Pyrrolyl-acetamino)-rutaecarpine Drug Info [530639]
3-(2-N-Pyrrolyl-propionamino)-rutaecarpine Drug Info [530639]
3-(dimethylamino)phenyl phenylcarbamate Drug Info [551218]
3-chlorophenyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
3-isopr-sal-cyclosal-d4TMP Drug Info [528706]
3-methoxyphenyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
3-phenyl-cyclosal-d4TMP Drug Info [528706]
3-sal-cyclosal-d4TMP Drug Info [528706]
3-[10-(benzylmethylamino)decyloxy]xanthen-9-one Drug Info [528456]
3-[11-(benzylmethylamino)undecyloxy]xanthen-9-one Drug Info [528456]
3-[12-(benzylmethylamino)dodecyloxy]xanthen-9-one Drug Info [528456]
3-[3-(benzylmethylamino)propoxy]xanthen-9-one Drug Info [528456]
3-[4-(benzylmethylamino)butoxy]xanthen-9-one Drug Info [528456]
3-[5-(benzylmethylamino)pentyloxy]xanthen-9-one Drug Info [528456]
3-[6-(benzylmethylamino)hexyloxy]xanthen-9-one Drug Info [528456]
3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-one Drug Info [528456]
3-[8-(benzylmethylamino)octyloxy]xanthen-9-one Drug Info [528456]
3-[9-(benzylmethylamino)nonyloxy]xanthen-9-one Drug Info [528456]
4-chlorophenyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
4-ISOPROPYLPHENSERINE Drug Info [530692]
4-methoxyphenyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
4-[4-(benzyloxy)piperidino]butyl benzoate Drug Info [528979]
4-[4-(benzyloxy)piperidino]butyl-3-chlorobenzoate Drug Info [528979]
4-[4-(benzyloxy)piperidino]butyl-3-fluorobenzoate Drug Info [528979]
4-[4-(benzyloxy)piperidino]butyl-4-chlorobenzoate Drug Info [528979]
4-[4-(benzyloxy)piperidino]butyl-4-fluorobenzoate Drug Info [528979]
4-[4-(benzyloxy)piperidino]butyl-4-nitrobenzoate Drug Info [528979]
5,6-dinitroacenaphthoquinone Drug Info [529103]
5-methyl-cyclosal-d4TMP Drug Info [528706]
6-chlorotacrine hydrochloride Drug Info [530301]
6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-ium Drug Info [528415]
6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-ium Drug Info [528415]
6-hydroxy-2-methyl-9H-beta-carbolin-2-ium Drug Info [528415]
6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-ium Drug Info [528415]
6-methoxy-1,9-dimethyl-9H-pyrido[3,4-b]indole Drug Info [528415]
6-methoxy-2-methyl-9H-beta-carbolin-2-ium Drug Info [528415]
7-Oxo-7H-dibenzo[de,g]quinoline Drug Info [529985]
9-(3-IODOBENZYLAMINO)-1,2,3,4-TETRAHYDROACRIDINE Drug Info [551374]
9-Ethyl-2-methyl-beta-carboline-2-ium iodide Drug Info [530824]
9-N-Phenylmethylamino-Tacrine Drug Info [551393]
9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromide Drug Info [530625]
9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromide Drug Info [530625]
9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromide Drug Info [530920]
9-O-[3-(4-Bromo-phenoxyl)butyl]-berberine bromide Drug Info [530920]
9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromide Drug Info [530920]
9-O-[3-(Phenylamino)propyl]-berberine bromide Drug Info [530920]
9-O-[3-(Phenylol-1-yloxy)propyl]berberine bromide Drug Info [530625]
9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromide Drug Info [530625]
9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromide Drug Info [530625]
9-[5-(beta-Carboline-9-yl)pentyl]-beta-carboline Drug Info [530824]
9-[9-(beta-Carboline-9-yl)nonyl]-beta-carboline Drug Info [530824]
ACENAPHTHOQUINONE Drug Info [529103]
Alpha-D-Mannose Drug Info [551393]
Anthracen-10-yl(10H-phenothiazin-10-yl)methanone Drug Info [528978]
AS-1397 Drug Info [528564]
BChE inhibitors Drug Info [543635]
BENZOQUINONE Drug Info [527510]
Beta-D-Mannose Drug Info [551393]
Bis-7-tacrine Drug Info [530923]
Bis-cyclosal-d4TMP Drug Info [528706]
Butanoic Acid Drug Info [551393]
Butyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
Butyrylthiocholine Drug Info [551391]
CAPROCTAMINE Drug Info [529775]
CHF-2819 Drug Info [527437]
CHLORANIL Drug Info [527510]
Cyclopentyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
Cyclosal-d4TMP Drug Info [528706]
Cymserine Drug Info [535406]
DEMETHYLDEBROMOFLUSTRAMINE B Drug Info [529633]
Diethylphosphono Group Drug Info [551393]
DODECANESULFONATE ION Drug Info [551374]
Ethyl Dihydrogen Phosphate Drug Info [551393]
ETHYL HYDROGEN DIETHYLAMIDOPHOSPHATE Drug Info [551374]
Fucose Drug Info [551393]
HALOXYSTEROL A Drug Info [527846]
HALOXYSTEROL B Drug Info [527846]
Haloxysterol C Drug Info [527846]
Haloxysterol D Drug Info [527846]
HEPTYPHYSOSTIGMINE Drug Info [528106]
Hexafluronium bromide Drug Info [537808]
Huprine X Drug Info [528216]
Huprine-Tacrine Heterodimer Drug Info [527471]
Iso-OMPA Drug Info [529716]
Isopropyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
Isosorbide-2-(benzylcarbamate)-5-benzoate Drug Info [529716]
Isosorbide-2-(benzylcarbamate)-5-mononitrate Drug Info [529716]
Isosorbide-2-(butylcarbamate)-5-benzoate Drug Info [529716]
Isosorbide-2-(butylcarbamate)-5-mononitrate Drug Info [529716]
Isosorbide-2-(cyclohexylcarbamate)-5-mononitrate Drug Info [529716]
Isosorbide-2-(ethylcarbamate)-5-mononitrate Drug Info [529716]
Isosorbide-2-(methylcarbamate)-5-benzoate Drug Info [529716]
Isosorbide-2-(methylcarbamate)-5-mononitrate Drug Info [529716]
Isosorbide-2-(propylcarbamate)-5-mononitrate Drug Info [529716]
Isosorbide-2-benzyl carbamate Drug Info [530632]
Isosorbide-2-benzylcarbamate-5-(o-toluate) Drug Info [530632]
Isosorbide-2-benzylcarbamate-5-acetate Drug Info [529716]
Isosorbide-2-benzylcarbamate-5-cyclopentanoate Drug Info [529716]
Isosorbide-2-benzylcarbamate-5-cyclopropanoate Drug Info [529716]
Isosorbide-2-benzylcarbamate-5-isonicotinate Drug Info [529716]
Isosorbide-2-benzylcarbamate-5-nicotinate Drug Info [529716]
Isosorbide-2-benzylcarbamate-5-pentanoate Drug Info [529716]
Isosorbide-2-benzylcarbamate-5-propionate Drug Info [529716]
Isosorbide-2-benzylcarbamate-5-triflate Drug Info [529716]
Isosorbide-di-(benzylcarbamate) Drug Info [530646]
Isosorbide-di-(butylcarbamate) Drug Info [530646]
Isosorbide-di-(ethylcarbamate) Drug Info [530646]
Isosorbide-di-(propylcarbamate) Drug Info [530646]
LAWSARITOL Drug Info [527846]
LIPOCRINE Drug Info [530437]
M-tolyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
MEMOQUIN Drug Info [530437]
MEPTAZINOL Drug Info [529368]
Methyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
Methyl Phosphinic Acid Drug Info [551393]
MF-8623 Drug Info [535406]
Monoisopropyl Ester Phosphonic Acid Group Drug Info [551393]
Morpholino(1'H-phenothiazin-1'-yl)methanone Drug Info [530749]
N,N'-(1',10'-decylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',11'-undecydene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',2'-ethylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',3'-propylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',4'-butylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',5'-pentylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',6-hexylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',7'-heptylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',8'-octylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N'-(1',9'-nonylene)-bis-(-)-nor-MEP Drug Info [529368]
N,N-Diethyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N,N-Diisopropyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N,N-Dimethyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N,N-Dipropyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-(Adamant-1-yl)-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-Benzyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-benzyl-2-thiomorpholinopyrimidin-4-amine Drug Info [530923]
N-Cyclobutyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-Cyclohexyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-Cyclopentyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-Isopropyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-Methyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-n-heptyl-7-methoxytacrine hydrochloride Drug Info [531150]
N-n-hexyl-7-methoxytacrine hydrochloride Drug Info [531150]
N-n-nonyl-7-methoxytacrine hydrochloride Drug Info [531150]
N-n-octyl-7-methoxytacrine hydrochloride Drug Info [531150]
N-n-pentyl-7-methoxytacrine hydrochloride Drug Info [531150]
N-Neopentyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-o-Tolyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-p-Tolyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-phenethyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine Drug Info [530923]
N-Phenyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
N-tert-Butyl-1'H-phenothiazine-1'-carboxamide Drug Info [530749]
Naphthalen-1-yl 10H-phenothiazine-10-carboxylate Drug Info [529548]
Naphthalen-1-yl(10H-phenothiazin-10-yl)methanone Drug Info [528978]
Naphthalen-2-yl 10H-phenothiazine-10-carboxylate Drug Info [529548]
Naphthalen-2-yl(10H-phenothiazin-10-yl)methanone Drug Info [528978]
NOSTOCARBOLINE Drug Info [527942]
NP-0336 Drug Info [543635]
NSC-23180 Drug Info [529103]
O-tolyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
P-tolyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
Phenanthrene-9,10-dione Drug Info [529103]
Phenyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
Tert-butyl 10H-phenothiazine-10-carboxylate Drug Info [529548]
TOLSERINE Drug Info [528106]
VAGANINE D Drug Info [526090]
XANTHOSTIGMINE Drug Info [534716]
Modulator JES-9501 Drug Info [525989]
Non-PEGylated butyrylcholinesterase Drug Info [543635]
Plasma derived human butyrylcholinesterase Drug Info [533276]
Protexia Drug Info [527984]
Recombinant human butyrylcholinesterase Drug Info [543635]
Pathways
PANTHER Pathway Muscarinic acetylcholine receptor 1 and 3 signaling pathway
Muscarinic acetylcholine receptor 2 and 4 signaling pathway
Nicotinic acetylcholine receptor signaling pathway
WikiPathways Irinotecan Pathway
References
Ref 521839ClinicalTrials.gov (NCT00333528) A Study of Plasma-Derived Human Butyrylcholinesterase Administered Intramuscularly. U.S. National Institutes of Health.
Ref 522424ClinicalTrials.gov (NCT00744146) First Time in Human Study of Protexia. U.S. National Institutes of Health.
Ref 525989Dehydroevodiamine attenuates beta-amyloid peptide-induced amnesia in mice. Eur J Pharmacol. 2001 Feb 16;413(2-3):221-5.
Ref 532220Neurotrophic and neuroprotective actions of (-)- and (+)-phenserine, candidate drugs for Alzheimer's disease. PLoS One. 2013;8(1):e54887.
Ref 537810Pharmacology, clinical uses, and adverse effects of ceruletide, a cholecystokinetic agent. Pharmacotherapy. 1982 Jul-Aug;2(4):223-34.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525989Dehydroevodiamine attenuates beta-amyloid peptide-induced amnesia in mice. Eur J Pharmacol. 2001 Feb 16;413(2-3):221-5.
Ref 526090J Nat Prod. 2001 Jun;64(6):842-4.Steroidal alkaloids from the leaves of Sarcococca coriacea of Nepalese origin.
Ref 527437J Med Chem. 2005 Feb 24;48(4):986-94.Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
Ref 527471J Med Chem. 2005 Mar 24;48(6):1701-4.Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.
Ref 527510J Med Chem. 2005 Apr 21;48(8):2906-15.Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.
Ref 527846Bioorg Med Chem Lett. 2006 Feb;16(3):573-80. Epub 2005 Nov 7.Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum.
Ref 527942J Nat Prod. 2005 Dec;68(12):1793-5.Nostocarboline: isolation and synthesis of a new cholinesterase inhibitor from Nostoc 78-12A.
Ref 527984In vitro and in vivo characterization of recombinant human butyrylcholinesterase (Protexia) as a potential nerve agent bioscavenger. Chem Biol Interact. 2005 Dec 15;157-158:363-5.
Ref 528106J Med Chem. 2006 Apr 6;49(7):2174-85.Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
Ref 528216J Med Chem. 2006 Jun 1;49(11):3421-5.Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites.
Ref 528402J Med Chem. 2006 Sep 7;49(18):5411-3.Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase.
Ref 528415Bioorg Med Chem Lett. 2006 Nov 15;16(22):5840-3. Epub 2006 Sep 1.6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
Ref 528456Bioorg Med Chem. 2007 Jan 1;15(1):575-85. Epub 2006 Sep 27.Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones.
Ref 528564J Med Chem. 2006 Dec 14;49(25):7540-4.Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase.
Ref 528570J Med Chem. 2006 Nov 16;49(23):6833-40.Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the oxyanion hole.
Ref 528706J Med Chem. 2007 Mar 22;50(6):1335-46. Epub 2007 Mar 1.Bis-cycloSal-d4T-monophosphates: drugs that deliver two molecules of bioactive nucleotides.
Ref 528749J Med Chem. 2007 Apr 19;50(8):1876-85. Epub 2007 Mar 23.Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
Ref 528766Bioorg Med Chem. 2007 Jun 1;15(11):3801-17. Epub 2007 Mar 12.Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.
Ref 528978Bioorg Med Chem. 2007 Oct 1;15(19):6367-78. Epub 2007 Jul 6.Selective reversible inhibition of human butyrylcholinesterase by aryl amide derivatives of phenothiazine.
Ref 528979Bioorg Med Chem. 2007 Oct 15;15(20):6596-607. Epub 2007 Jul 25.Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics.
Ref 529103J Med Chem. 2007 Nov 15;50(23):5727-34. Epub 2007 Oct 17.Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1.
Ref 529368J Med Chem. 2008 Apr 10;51(7):2027-36. Epub 2008 Mar 12.Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
Ref 529473J Med Chem. 2008 Jun 12;51(11):3154-70. Epub 2008 May 15.Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
Ref 529548J Med Chem. 2008 Jul 24;51(14):4200-12. Epub 2008 Jun 21.Carbamates with differential mechanism of inhibition toward acetylcholinesterase and butyrylcholinesterase.
Ref 529633J Med Chem. 2008 Sep 11;51(17):5271-84. Epub 2008 Aug 8.Synthesis and biological evaluation of (-)- and (+)-debromoflustramine B and its analogues as selective butyrylcholinesterase inhibitors.
Ref 529716J Med Chem. 2008 Oct 23;51(20):6400-9. Epub 2008 Sep 26.Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
Ref 529775J Med Chem. 2008 Nov 27;51(22):7308-12.Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
Ref 529985Eur J Med Chem. 2009 Jun;44(6):2523-32. Epub 2009 Jan 31.Synthesis, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinesterase/butyrylcholinesterase.
Ref 530301J Med Chem. 2009 Sep 10;52(17):5365-79.Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
Ref 530437J Med Chem. 2009 Dec 10;52(23):7883-6.Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
Ref 530625Bioorg Med Chem. 2010 Feb;18(3):1244-51. Epub 2009 Dec 16.Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors.
Ref 530632J Med Chem. 2010 Feb 11;53(3):1190-9.Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
Ref 530639Eur J Med Chem. 2010 Apr;45(4):1415-23. Epub 2010 Jan 4.Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors.
Ref 530646Bioorg Med Chem. 2010 Feb;18(3):1045-53. Epub 2010 Jan 6.Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability.
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