Obidoxime Chloride: Cholinesterase reactivator occurring in two interchangeable isomeric forms, syn and anti. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 8250 |
| MeSH ID | M0015162 |
| PubMed CID | 135566074 |
| MeSH ID | M0015162 |
| Synonym |
|---|
| obidoxime chloride |
| 114-90-9 |
| FT-0631656 |
| bis(4-hydroxyiminomethyl-1-pyridiniomethyl)ether dichloride |
| 1,1'-[oxybis(methylene)]bis[4-(hydroxyimino) methyl]pyridinium dichloride |
| lueh 6 |
| 1,3-bis(4-aldoximinopyridinium) dimethyl ether bichloride |
| einecs 204-059-5 |
| pyridinium, 1,1'-(oxybis(methylene))bis(4-(hydroxyimino)methyl)-, dichloride |
| toksobidin |
| obidoximi chloridum [inn-latin] |
| cloruro de obidoxima [inn-spanish] |
| bis(isonicotinaldoxime 1-methyl) ether dichloride |
| ether bis-14-hydroxy-iminomethylopyridine-(1)-metylodichloride [polish] |
| obidoxime dichloride |
| chlorure d'obidoxime [inn-french] |
| 1,3-bis(4-hydroxyiminomethyl-1-pyridinio)-2-oxapropane dichloride |
| 1,1'-(oxydimethylene)bis(4-formylpyridinium)dichloride dioxime |
| n,n-dimethyleneoxidebis(pyridinium-4-aldoxime) dichloride |
| luh(sub 6) |
| pyridinium, 1,1'-(oxydimethylene)bis(4-formyl-, dichloride, dioxime |
| 1,1'-(oxydimethylene)bis(4-formylpyridinium) dioxime dichloride |
| obidoxime hydrochloride |
| 1,1'-(oxydimethylene)bis(4-formylpyridinium) dichloride dioxime |
| toxogonine |
| 1,1'-(oxybis(methylene))bis(4-(hydroxyimino)methyl)pyridinium dichloride |
| obidoxime chloride [usan:inn] |
| luh6 |
| bis(4-hydroxyiminomethylpyridinium-1-methyl)ether dichloride |
| n,n-dimethylenoxid-bis-(pyridinium-4-aldoxim)-dichlorid [german] |
| D05215 |
| obidoxime chloride (usan) |
| obidoxime chloride, >=95.0% (hplc) |
| nsc-757237 |
| 3hxr312z9m , |
| n,n-dimethylenoxid-bis-(pyridinium-4-aldoxim)-dichlorid |
| cloruro de obidoxima |
| ether bis-14-hydroxy-iminomethylopyridine-(1)-metylodichloride |
| chlorure d'obidoxime |
| obidoximi chloridum |
| unii-3hxr312z9m |
| nsc 757237 |
| toxogonin dichloride |
| obidoxime chloride [usan] |
| obidoxime chloride [mart.] |
| obidoxime chloride [inn] |
| obidoxime chloride [who-dd] |
| obidoxime chloride [mi] |
| AKOS025397238 |
| J-003154 |
| obidoxime chloride, analytical reference material |
| pyridinium, 1,1'-[oxybis(methylene)]bis[4-[(hydroxyimino)methyl]-, chloride (1:2) |
| AKOS030241577 |
| obidoximchlorid |
| 1,1-[oxybis(methylene)]bis[4-(hydroxyimino) methyl]pyridinium dichloride |
| 1,1'-(oxybis(methylene))bis(4-((hydroxyimino)methyl)pyridin-1-ium) chloride |
| obidoxime (dichloride) |
| CS-W011824 |
| HY-W011108 |
| 1,1'-(oxybis(methylene))bis(4-((hydroxyimino)methyl)pyridin-1-ium)chloride |
| 1,1'[oxybis(methylene)]-bis[4-(hydroxyimino)methyl]pyridinium dichloride |
| Excerpt | Reference | Relevance |
|---|---|---|
| " It was established that both for rats and for sheep and lambs T was almost twice as toxic as 2-PAM." | ( [Toxicity of oximes and their effect on acetylcholinesterase activity in the blood and myoneural synapses of animals]. Georgiev, B; Khristoskova, E, 1978) | 0.26 |
| "A comparative characteristic of acute toxicity of toxogonine and dipiroxime is given for different animal species with various routes of introduction of the compounds from which it follows that, as concerns the toxicity parameters and the area of toxic action, toxogonine is in the lead." | ( [Toxicity and tolerance of toxogonin]. Arestova, LS; Gurina, EI; Smirnova, OI; Zhigalova, LV, ) | 0.13 |
| " Maximum protection, as determined by a shift of the LD50 for the two OP agents, was observed with the cholinolytic benactyzine." | ( Actions and interactions of cholinolytics and cholinesterase reactivators in the treatment of acute organophosphorus toxicity. Asthana, SN; Batra, BS; Chowdhri, BL; Das Gupta, S; Ghosh, AK, 1991) | 0.28 |
| "The therapeutic efficacy of the new asymmetric bispyridinium oxime BI-6 against acute toxicity of the highly toxic organophosphate soman and the organophosphorus insecticide fosdrin by means of affecting the LD50 values of these noxiores substances was compared with the effect of the hitherto most perspective oxime HI-6 and the classic obidoxime always in combination with the identical dose of atropine." | ( [Comparison of the effects of BI-6, a new asymmetric bipyridine oxime, with HI-6 oxime and obidoxime in combination with atropine on soman and fosdrine toxicity in mice]. Kassa, J, 1999) | 0.3 |
| " The consistently steep probit slopes of the dose-response curves for highly toxic OP compounds suggested that these compounds have a single specific mechanism of toxicity regardless of the OP compound or the species in which it was tested." | ( Acetylcholinesterase inhibition: does it explain the toxicity of organophosphorus compounds? Brecht, KM; Koplovitz, I; Maxwell, DM; Sweeney, RE, 2006) | 0.33 |
| "The potency of newly developed oximes (K074, K075) and commonly used oximes (obidoxime, trimedoxime, and HI-6) to counteract tabun or cyclosarin-induced acute toxic effects was studied in mice." | ( A comparison of the potency of newly developed oximes (K074, K075) and currently available oximes (obidoxime, trimedoxime, HI-6) to counteract acute toxic effects of tabun and cyclosarin in mice. Humlicek, V; Kassa, J, 2008) | 0.35 |
| " Our LD50 data show that K-107, K-108 and K-113 (which strongly inhibit AChE in vitro) are in vivo markedly more toxic than all other oximes tested and can therefore only be safely administered at a low dosage which is insufficient to protect from DFP-induced mortality." | ( Eight new bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from diisopropylfluorophosphate toxicity. Hasan, MY; Kuca, K; Lorke, DE; Musilek, K; Nurulain, SM; Petroianu, GA, 2008) | 0.35 |
| " In the ED50 study, male guinea pigs clipped of hair received 2x LD50 topical challenges of undiluted Russian VX (VR), VX, or phorate oxon (PHO) and, at the onset of cholinergic signs, IM therapy of atropine (0." | ( Toxicity and median effective doses of oxime therapies against percutaneous organophosphorus pesticide and nerve agent challenges in the Hartley guinea pig. Babin, MC; Jett, DA; Platoff, GE; Snider, TH; Yeung, DT, 2016) | 0.43 |
| " We further evaluated the efficacy of two different antidotal regimens, one comprising a single and the other repeated administration of antidotes, in countering the toxic effects of the exposure." | ( Repetitive antidotal treatment is crucial in eliminating eye pathology, respiratory toxicity and death following whole-body VX vapor exposure in freely moving rats. Bloch-Shilderman, E; Cohen, L; Egoz, I; Gez, R; Gutman, H; Nili, U; Rabinovitz, I; Yacov, G, 2019) | 0.51 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The elimination half-life ranged from 35 min in normal rats to 86 min in sarin-poisoned rats." | ( Pharmacokinetics and pharmacodynamics of obidoxime in sarin-poisoned rats. Alioth-Streichenberg, CM; Bodmer, DM; Waser, PG, 1991) | 0.28 |
| " Possible reasons for the different pharmacokinetic values as compared with values previously reported in healthy volunteers are discussed." | ( Pharmacokinetics of obidoxime in organophosphate poisoning associated with renal failure. Bentur, Y; Nutenko, I; Raikhlin-Eisenkraft, B; Taitelman, U; Tsipiniuk, A, 1993) | 0.29 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " PANPAL pretreatment did not improve the efficacy of HI-6 in combination with benactyzine on soman-induced anticholinesterase and stressogenic effects." | ( The influence of pharmacological pretreatment on efficacy of HI-6 oxime in combination with benactyzine in soman poisoning in rats. Bajgar, J; Kassa, J, 1996) | 0.29 |
| "The therapeutic efficacy of the new asymmetric bispyridinium oxime BI-6 against acute toxicity of the highly toxic organophosphate soman and the organophosphorus insecticide fosdrin by means of affecting the LD50 values of these noxiores substances was compared with the effect of the hitherto most perspective oxime HI-6 and the classic obidoxime always in combination with the identical dose of atropine." | ( [Comparison of the effects of BI-6, a new asymmetric bipyridine oxime, with HI-6 oxime and obidoxime in combination with atropine on soman and fosdrine toxicity in mice]. Kassa, J, 1999) | 0.3 |
| "The effect of three newly developed bispyridinium non-oxime compounds (MB408, MB442, and MB444) on the therapeutic efficacy of a standard antidotal treatment (atropine in combination with the oxime HI-6 or obidoxime) of acute poisoning by two nerve agents (sarin and cyclosarin) in mice was studied." | ( Some benefit from non-oximes MB408, MB442 and MB444 in combination with the oximes HI-6 or obidoxime and atropine in antidoting sarin or cyclosarin poisoned mice. Bird, M; Green, AC; Kassa, J; Tattersall, JEH; Timperley, CM; Williams, RL, 2018) | 0.48 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Rapid reactivation of OP-hBChE conjugates by uncharged and nonprotonated tertiary imidazole aldoximes allows the design of a new OP countermeasure by conversion of hBChE from a stoichiometric to catalytic OP bioscavenger with the prospect of oral bioavailability and central nervous system penetration." | ( Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification. Amitai, G; Fokin, VV; Radić, Z; Sharpless, KB; Sit, RK; Taylor, P, 2014) | 0.4 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " We conclude that each drug should be titrated separately: atropine dosage should be adjusted to the severity of tracheobronchial secretions and bronchospasm, while full doses of obidoxime are justified for the period before "aging" sets in." | ( Antidotal therapy of severe acute organophosphate poisoning: a multihospital study. Finkelstein, Y; Kushnir, A; Raikhlin-Eisenkraft, B; Taitelman, U, ) | 0.13 |
| " 4 The kinetic data of reactivation established for diethylphosphoryl-AChE of human red cells indicate that the usually recommended dosage to attain a plasma concentration of 4 micrograms/ml does not permit exploitation of the full therapeutic potential of the oximes, in particular of pralidoxime." | ( Reappraisal of indications and limitations of oxime therapy in organophosphate poisoning. Bäcker, M; Eyer, P; Klimmek, R; Mast, U; Szinicz, L; Thiermann, H; Worek, F, 1997) | 0.3 |
| " Assuming that the tails of dose-response curves of toxicity for bisquaternary oximes are shallow and similar to one another, one could substitute the ED(10) for the MTD." | ( Determination of therapeutic doses of bisquaternary oximes in large animals. Adani, R; Amitai, G; Chen, R; Cohen, G; Rabinovitz, I; Raveh, L; Zomber, G, ) | 0.13 |
| " Varying dosage schedules of pralidoxime or obidoxime were used." | ( Oxime therapy and outcomes in human organophosphate poisoning: an evaluation using meta-analytic techniques. Graham, P; Moran, JL; Peter, JV, 2006) | 0.33 |
| " Mortality dose-response curves for several OP compounds (i." | ( Acetylcholinesterase inhibition: does it explain the toxicity of organophosphorus compounds? Brecht, KM; Koplovitz, I; Maxwell, DM; Sweeney, RE, 2006) | 0.33 |
| " Our LD50 data show that K-107, K-108 and K-113 (which strongly inhibit AChE in vitro) are in vivo markedly more toxic than all other oximes tested and can therefore only be safely administered at a low dosage which is insufficient to protect from DFP-induced mortality." | ( Eight new bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from diisopropylfluorophosphate toxicity. Hasan, MY; Kuca, K; Lorke, DE; Musilek, K; Nurulain, SM; Petroianu, GA, 2008) | 0.35 |
| " Both synthetic mixtures and dosage forms were assayed." | ( A quantitative NMR protocol for the simultaneous analysis of atropine and obidoxime in parenteral injection devices. Dubey, DK; Ganesan, K; Gupta, PK; Mazumder, A; Sharma, R; Vijayaraghavan, R, 2009) | 0.35 |
| " Rats received paraoxon in a dosage of 1, 5, or 10 mumol, and immediately thereafter intraperitoneal injections of the respective oxime at a dosage of half the LD(01)." | ( Efficacy of eight experimental bispyridinium oximes against paraoxon-induced mortality: comparison with the conventional oximes pralidoxime and obidoxime. Hasan, MY; Kuca, K; Lorke, DE; Musilek, K; Nurulain, SM; Petroianu, GA; Shafiullah, M, 2009) | 0.35 |
| " Rats received DFP intraperitoneally in a dosage of 6, 8, or 10 micromol/rat and immediately thereafter intraperitoneal injections of K-27, K-48, pralidoxime, obidoxime, trimedoxime, methoxime, or HI-6." | ( Efficacy of two new asymmetric bispyridinium oximes (K-27 and K-48) in rats exposed to diisopropylfluorophosphate: comparison with pralidoxime, obidoxime, trimedoxime, methoxime, and HI-6. Hasan, MY; Kuca, K; Lorke, DE; Nurulain, SM; Petroianu, GA; Schmitt, A, 2009) | 0.35 |
| " Thus, the data presented strongly support the administration of appropriately dosed oximes, preferably obidoxime, in paraoxon-poisoned patients to restore paraoxon-impaired muscle force." | ( Muscle force and acetylcholinesterase activity in mouse hemidiaphragms exposed to paraoxon and treated by oximes in vitro. Eyer, P; Thiermann, H; Worek, F, 2010) | 0.36 |
| " Furthermore, we investigated the therapeutic efficacy of a single dose of atropine, obidoxime and diazepam, administered at appearance of first clinical signs, versus that of repetitive dosing of these drugs on the reappearance of signs." | ( Percutaneous exposure to the nerve agent VX: Efficacy of combined atropine, obidoxime and diazepam treatment. Joosen, MJ; van der Schans, MJ; van Helden, HP, 2010) | 0.36 |
| " Thus, the present study aimed to investigate the time-course and dose-response efficacy of a brief 4min isoflurane administration as a treatment for neurotoxicity induced by OP-CTA." | ( Brief isoflurane administration as a post-exposure treatment for organophosphate poisoning. Appu, AP; Arun, P; Braga, MF; Figueiredo, TH; Flagg, T; Krishnan, JKS; Moffett, JR; Namboodiri, AM; Puthillathu, N, 2017) | 0.46 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cholinesterase | Homo sapiens (human) | IC50 (µMol) | 1,910.0000 | 0.0000 | 1.5599 | 10.0000 | AID551379 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 (µMol) | 964.0000 | 0.0000 | 0.9332 | 10.0000 | AID1140219; AID1173386; AID1311977; AID1826689; AID551378; AID552421 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Acetylcholinesterase | Homo sapiens (human) | Kd | 124.6629 | 0.0080 | 1.7750 | 5.3000 | AID1140212; AID1140213; AID1173380; AID1173381; AID1173382; AID1311971; AID1311972; AID1471800; AID1471803; AID1471806; AID1471809; AID710208; AID710209; AID710210 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Acetylcholinesterase | Homo sapiens (human) | Kdiss | 63.0000 | 5.0000 | 5.0000 | 5.0000 | AID1859554; AID1859575 |
| Acetylcholinesterase | Rattus norvegicus (Norway rat) | KR | 3.0000 | 3.0000 | 4.5000 | 6.0000 | AID302661 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1140213 | Binding affinity to VX-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate measured up to 1 hr by Ellman method | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1131011 | Reduction of diisopropyl fluorophosphate-induced hypothermia in rat at 80 mg/kg, ip administered 1 hr after diisopropyl fluorophosphate-challenge measured after 3 to 4 hrs relative to control | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID364612 | Reactivation of 10 uM tabun inhibited AChE in rat brain homogenate | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID302659 | Reactivation activity of tabun-inhibited AChE in rat brain at 10 uM after 30 mins | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). |
| AID1471804 | Reactivation of cyclosarin inhibited human erythrocyte AChE assessed as overall bimolecular reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's me | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID552421 | Inhibition of human recombinant AChE by modified Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID615412 | Reactivation of VX-inhibited electric eel AChE activity after 40 mins by Ellman's method relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID1173379 | Reactivation of tabun-inhibited human acetylcholinesterase assessed as reactivation rate constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID30830 | Maximal displacement of GD from acetylcholinesterase (AChE) of bovine erythrocytes | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases. |
| AID1471806 | Reactivation of tabun inhibited human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1130961 | Half life in guinea pig blood at 25 mg/kg, iv by spectrophotometric analysis | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID710209 | Binding affinity to tabun-human AChE complex | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID352067 | Reactivation of sarin-inhibited electric eel AChE at 100 uM after 10 mins by Ellman's method relative to control | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker. |
| AID1173374 | Reactivation of VX-inhibited human acetylcholinesterase at 0.1 mM in pH 7.4 phosphate buffer at 37 degC by Ellman's method | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID1311976 | Reactivation of VX-inhibited hemoglobin free erythrocyte ghost human AChE assessed as second order rate constant using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1130958 | Half life in WAG rat blood at 25 mg/kg, iv by spectrophotometric analysis | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID615414 | Dissociation constant, pKa of the compound by spectrophotometric analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID1130951 | Reactivation of sarin-inhibited bovine erythrocyte AChE assessed as restored enzyme activity at 1 mM at pH 7.5 after 3 mins relative to control | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID302658 | Reactivation activity of tabun-inhibited AChE in rat brain at 100 uM after 30 mins | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). |
| AID1173378 | Reactivation of VX-inhibited human acetylcholinesterase assessed as reactivation rate constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID276245 | Reactivation of tabun inhibited AChE from rat brain at 1 mM | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. |
| AID551378 | Inhibition of human recombinant AChE | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Preparation, in vitro screening and molecular modelling of symmetrical 4-tert-butylpyridinium cholinesterase inhibitors--analogues of SAD-128. |
| AID302657 | Reactivation activity of tabun-inhibited AChE in rat brain at 1 mM after 30 mins | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). |
| AID615404 | Reactivation of sarin-inhibited electric eel AChE activity at 0.001 M and pH 8 after 10 mins by Ellman's method relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID1173377 | Reactivation of sarin-inhibited human acetylcholinesterase assessed as reactivation rate constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID32126 | First-order rate constant for acetylcholinesterase was determined in vitro in rat brain | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis of a new reactivator of tabun-inhibited acetylcholinesterase. |
| AID1130956 | Half life in hybrid CC57 mouse blood at 25 mg/kg, iv by spectrophotometric analysis | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID1859588 | Reactivation of tabun induced inhibition of BChE in human plasma assessed as second-order rate constant using ATCh as substrate incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID615405 | Reactivation of sarin-inhibited electric eel AChE activity at 0.0001 M and pH 8 after 10 mins by Ellman's method relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID710212 | Reactivation of VX-inhibited human AChE assessed as bimolecular reactivation rate constant | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID1311971 | Binding affinity to sarin-inhibited hemoglobin free erythrocyte ghost human AChE using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1131007 | Reduction of diisopropyl fluorophosphate-induced hypothermia in rat at 150 mg/kg, ip administered 1 hr after diisopropyl fluorophosphate-challenge measured after 3 to 4 hrs relative to control | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID1859554 | Reactivation of tabun induced inhibition of recombinant human AChE assessed as dissociation constant using ATCh as substrate incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID392539 | Reactivation of paraoxon-inhibited house fly AChE at 5 mM after 1 hr | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | Reactivation potency of fluorinated pyridinium oximes for acetylcholinesterases inhibited by paraoxon organophosphorus agent. |
| AID301221 | Reactivation of 0.1 uM tabun-inhibited rat brain AchE | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21 | Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID1826698 | Reactivation of NEDPA-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, Kr2 by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1859600 | Reactivation of tabun induced inhibition of BChE in human plasma assessed as time needed to achieve maximal reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID552414 | Reactivation of GA-mediated inactive human recombinant AChE at 10 uM after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID1311972 | Binding affinity to VX-inhibited hemoglobin free erythrocyte ghost human AChE using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID31640 | Compound was evaluated for reactivation of para-nitrophenyl methylphosphate (EPMP)-phosphonylated human erythrocyte AChE at pH 7.6 | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Nonquaternary cholinesterase reactivators. 4. Dialkylaminoalkyl thioesters of alpha-keto thiohydroximic acids as reactivators of ethyl methylphosphonyl- and 1,2,2-trimethylpropyl methylphosphonyl-acetylcholinesterase in vitro. |
| AID307194 | Reactivation of 1000 uM paraoxon-induced inhibition of AChE in rat brain at pH 7.6 after 10 mins | 2007 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11 | Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. |
| AID1130963 | Half life in Flemish Giant rabbit blood at 25 mg/kg, iv by spectrophotometric analysis | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID615411 | Reactivation of diisopropyl phosphorofluoridate-inhibited electric eel AChE activity after 40 mins by Ellman's method relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID710205 | Reactivation of paraoxon-inhibited human AChE assessed as bimolecular reactivation rate constant | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID1173385 | Reactivation of tabun-inhibited human acetylcholinesterase assessed as second order reactivation rate constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID1471799 | Reactivation of sarin inhibited human erythrocyte AChE assessed as reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID392540 | Reactivation of paraoxon-inhibited bovine red blood cellular AChE at 5 mM after 1 hr | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4 | Reactivation potency of fluorinated pyridinium oximes for acetylcholinesterases inhibited by paraoxon organophosphorus agent. |
| AID1859580 | Reactivation of tabun induced inhibition of BChE in human plasma assessed as first-order reactivation rate constant using ATCh as substrate incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID89258 | Concentration of the HOX that inhibits 50% of AChE (Acetylcholinesterase) activity | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole. |
| AID31635 | Maximum reactivation for GD-inhibited human erythrocyte (RBC) AChE by oximes | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Nonquaternary cholinesterase reactivators. 4. Dialkylaminoalkyl thioesters of alpha-keto thiohydroximic acids as reactivators of ethyl methylphosphonyl- and 1,2,2-trimethylpropyl methylphosphonyl-acetylcholinesterase in vitro. |
| AID1826693 | Reactivation of NIMP-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, Kr by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1826690 | Reactivation of NEMP-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, Kr by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1173376 | Reactivation of tabun-inhibited human acetylcholinesterase at 0.1 mM in pH 7.4 phosphate buffer at 37 degC by Ellman's method | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID307193 | Reactivation of 10 uM tabun-induced inhibition of AChE in rat brain at pH 7.6 after 10 mins | 2007 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11 | Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. |
| AID1173383 | Reactivation of sarin-inhibited human acetylcholinesterase assessed as second order reactivation rate constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID1471802 | Reactivation of cyclosarin inhibited human erythrocyte AChE assessed as reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1173375 | Reactivation of tabun-inhibited human acetylcholinesterase at 1 mM in pH 7.4 phosphate buffer at 37 degC by Ellman's method | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID1471809 | Reactivation of VX inhibited human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1826699 | Reactivation of PARAOXON-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, Kr by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID31651 | Reactivation of para-nitrophenyl methylyphosphate (EPMP)-phosphonylated human erythrocyte AChE | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Nonquaternary cholinesterase reactivators. 4. Dialkylaminoalkyl thioesters of alpha-keto thiohydroximic acids as reactivators of ethyl methylphosphonyl- and 1,2,2-trimethylpropyl methylphosphonyl-acetylcholinesterase in vitro. |
| AID1311977 | Inhibition of hemoglobin free erythrocyte ghost human AChE using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID615407 | Reactivation of diisopropyl phosphorofluoridate-inhibited electric eel AChE activity at 0.0001 M and pH 8 after 10 mins by Ellman's method relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID552418 | Reactivation of MePOX-mediated inactive human recombinant AChE at 10 uM after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID1173372 | Reactivation of sarin-inhibited human acetylcholinesterase at 0.1 mM in pH 7.4 phosphate buffer at 37 degC by Ellman's method | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID68458 | The compound was tested for % of maximum reactivation for GD-inhibited Eel AChE (Acetylcholinesterase) by oximes | 1984 | Journal of medicinal chemistry, Nov, Volume: 27, Issue:11 | Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole. |
| AID1826696 | Reactivation of NEDPA-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, Kr by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1826691 | Reactivation of NEMP-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, KD by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1140212 | Binding affinity to sarin-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate measured up to 1 hr by Ellman method | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1173371 | Reactivation of sarin-inhibited human acetylcholinesterase at 1 mM in pH 7.4 phosphate buffer at 37 degC by Ellman's method | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID302660 | Toxicity in intramuscular dosed rat after 24 hrs | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). |
| AID1173384 | Reactivation of VX-inhibited human acetylcholinesterase assessed as second order reactivation rate constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID307195 | Reactivation of 10 uM paraoxon-induced inhibition of AChE in rat brain at pH 7.6 after 10 mins | 2007 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11 | Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. |
| AID1859562 | Reactivation of tabun induced inhibition of recombinant human AChE assessed as second-order reactivation rate constant using ATCh as substrate incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID32125 | In vitro dissociation constant of rat brain Acetylcholinesterase (AChE) inhibitor reactivator complex was determined | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis of a new reactivator of tabun-inhibited acetylcholinesterase. |
| AID1471808 | Reactivation of VX inhibited human erythrocyte AChE assessed as reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1311974 | Reactivation of VX-inhibited hemoglobin free erythrocyte ghost human AChE assessed as rate constant for cleavage of P-O bond of VX-AChE conjugate using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1140218 | Reactivation of VX-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate assessed as second order rate constant measured up to 1 hr by Ellman method | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1859574 | Reactivation of tabun induced inhibition of recombinant human AChE assessed as maximal first-order reactivation rate constant using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID364611 | Reactivation of 1000 uM tabun inhibited AChE in rat brain homogenate | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID1140216 | Acidic dissociation constant, pKa of the compound in phosphate/tris/glycine-NaOH containing buffer by UV-vis spectrophotometric analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID615406 | Reactivation of diisopropyl phosphorofluoridate-inhibited electric eel AChE activity at 0.001 M and pH 8 after 10 mins by Ellman's method relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID551379 | Inhibition of human recombinant BChE | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Preparation, in vitro screening and molecular modelling of symmetrical 4-tert-butylpyridinium cholinesterase inhibitors--analogues of SAD-128. |
| AID301220 | Reactivation of 1 mM paraoxon-inhibited rat brain AchE | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21 | Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID31634 | Percentage of maximum reactivation of GD-inhibited human erythrocyte acetylcholinesterase (AChE) | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases. |
| AID1826700 | Reactivation of PARAOXON-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, KD by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID407789 | Reactivation of rat brain AChE | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors. |
| AID1826695 | Reactivation of NIMP-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, Kr2 by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID650705 | Dissociation constant, pKa of the compound | 2011 | Journal of medicinal chemistry, May-12, Volume: 54, Issue:9 | Amidine-oximes: reactivators for organophosphate exposure. |
| AID552417 | Reactivation of MePOX-mediated inactive human recombinant AChE at 100 uM after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID364799 | Plasma concentration in human | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID1130966 | Half life in goat blood at 25 mg/kg, iv by spectrophotometric analysis | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID1826697 | Reactivation of NEDPA-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, KD by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1173373 | Reactivation of VX-inhibited human acetylcholinesterase at 1 mM in pH 7.4 phosphate buffer at 37 degC by Ellman's method | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID710210 | Binding affinity to VX-human AChE complex | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID1471801 | Reactivation of sarin inhibited human erythrocyte AChE assessed as overall bimolecular reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID364614 | Reactivation of 10 uM paraoxon inhibited AChE in rat brain homogenate | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID551380 | Selectivity index, ratio of IC50 for human recombinant BChE to IC50 for human recombinant AChE | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | Preparation, in vitro screening and molecular modelling of symmetrical 4-tert-butylpyridinium cholinesterase inhibitors--analogues of SAD-128. |
| AID1826701 | Reactivation of PARAOXON-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, Kr2 by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID552413 | Reactivation of GA-mediated inactive human recombinant AChE at 100 uM after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID1859576 | Reactivation of tabun induced inhibition of recombinant human AChE assessed as time needed to achieve maximal reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID30841 | Percentage of maximum reactivation of GD-inhibited AChE activity in eel | 1989 | Journal of medicinal chemistry, Feb, Volume: 32, Issue:2 | Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases. |
| AID552415 | Reactivation of POX-mediated inactive human recombinant AChE at 100 uM after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID364613 | Reactivation of 1000 uM paraoxon inhibited AChE in rat brain homogenate | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID1859592 | Reactivation of tabun induced inhibition of BChE in human plasma assessed as maximal first-order reactivation rate constant using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID1076758 | Reactivation of paraoxon OP-inactivated human plasma BChE assessed as reactivation rate constant using acetylthiocholine as substrate at 0.67 mM by spectrophotometric analysis | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification. |
| AID710207 | Reactivation of tabun-inhibited human AChE assessed as bimolecular reactivation rate constant | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID32127 | Bimolecular constants of reactivation was determined by its ability to reactivate tabun-inhibited AchE. | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis of a new reactivator of tabun-inhibited acetylcholinesterase. |
| AID1826689 | Inhibition of recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells using acetylthiocholine iodide as substrate measured for 6 mins by Ellman's method | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1471810 | Reactivation of VX inhibited human erythrocyte AChE assessed as overall biomolecular reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID301219 | Reactivation of 1 mM tabun-inhibited rat brain AchE | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21 | Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID1130952 | Competitive inhibition of bovine erythrocyte AChE using acetylcholine as substrate at 80 uM at pH 7.5 relative to control | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID1826708 | Permeability coefficient of compound in human BLEC monolayers assessed as radiolabeled 14C-D-glucose levels at 50 uM incubated for 1 hr by mass spectroscopy followed by scintillation counting method | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1471803 | Reactivation of cyclosarin inhibited human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1859543 | Reactivation of tabun induced inhibition of recombinant human AChE assessed as maximal first-order reactivation rate constant using ATCh as substrate incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID276248 | Reactivation of paraoxon inhibited AChE from rat brain at 0.1 uM | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. |
| AID260333 | Reactivation potency against inhibited AChE from rat brain homogenate at 0.01 mM | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase. |
| AID1140219 | Inhibition of hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate measured up to 1 hr by Ellman method | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID710211 | Reactivation of VX-inhibited human AChE assessed as reactivation rate constant | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID1311975 | Reactivation of sarin-inhibited hemoglobin free erythrocyte ghost human AChE assessed as second order rate constant using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1311973 | Reactivation of sarin-inhibited hemoglobin free erythrocyte ghost human AChE assessed as rate constant for cleavage of P-O bond of sarin-AChE conjugate using acetylcholine iodide as substrate measured for 1 hr by spectrophotometry based Ellman method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1140217 | Reactivation of sarin-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate assessed as second order rate constant measured up to 1 hr by Ellman method | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1076760 | Reactivation of OP-inactivated human plasma BChE using acetylthiocholine as substrate at 0.67 mM by spectrophotometric analysis | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification. |
| AID615409 | Reactivation of VX-inhibited electric eel AChE activity at 0.0001 M and pH 8 after 10 mins by Ellman's method relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID1826692 | Reactivation of NEMP-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, Kr2 by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID710208 | Binding affinity to paraoxon-human AChE complex | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID351913 | Reactivation of diisopropyl phosphorofluoridate-induced electric eel AChE inhibition at 1 mM by Ellman's method | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and evaluation of novel bis-pyridinium oximes as reactivators of DFP-inhibited acetylcholinesterase. |
| AID301222 | Reactivation of 0.1 uM paraoxon-inhibited rat brain AchE | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21 | Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase. |
| AID1826703 | Protective index of reactivation of NEMP-inhibited AChE in Swiss mouse at 100 umol/kg, ip treated for 1 min after paraoxon exposure by Dixon's up-and-down method relative to paraoxon alone | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID1471807 | Reactivation of tabun inhibited human erythrocyte AChE assessed as overall biomolecular reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1859584 | Reactivation of tabun induced inhibition of BChE in human plasma assessed as dissociation constant using ATCh as substrate incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID1859575 | Reactivation of tabun induced inhibition of recombinant human AChE assessed as maximal achieved reactivation using ATCh as substrate at 100 uM incubated for 30 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID710206 | Reactivation of paraoxon-inhibited human AChE assessed as reactivation rate constant | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID1140215 | Reactivation of VX-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate assessed as rate constant for displacement of phosphoryl residue from phosphorylated enzyme-compound complex measured up t | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1076756 | Reactivation of VX OP-inactivated human plasma BChE assessed as reactivation rate constant using acetylthiocholine as substrate at 0.67 mM by spectrophotometric analysis | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification. |
| AID1471800 | Reactivation of sarin inhibited human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1131012 | Reduction of paraoxon-induced hypothermia in rat at 80 mg/kg, ip administered 1 hr after paraoxon-challenge measured after 3 to 4 hrs relative to control | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID276247 | Reactivation of paraoxon inhibited AChE from rat brain at 1 mM | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. |
| AID276246 | Reactivation of tabun inhibited AChE from rat brain at 0.1 uM | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. |
| AID1859596 | Reactivation of tabun induced inhibition of BChE in human plasma assessed as maximal achieved reactivation using ATCh as substrate at 1 mM incubated for 30 mins by Ellman's method relative to control | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Halogen substituents enhance oxime nucleophilicity for reactivation of cholinesterases inhibited by nerve agents. |
| AID710213 | Reactivation of tabun-inhibited human AChE assessed as reactivation rate constant | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23 | Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase. |
| AID1173380 | Reactivation of sarin-inhibited human acetylcholinesterase assessed as dissociation constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID552416 | Reactivation of POX-mediated inactive human recombinant AChE at 10 uM after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID1140214 | Reactivation of sarin-inhibited hemoglobin free human erythrocyte ghost acetylcholinesterase using acetylthiocholineiodide as substrate assessed as rate constant for displacement of phosphoryl residue from phosphorylated enzyme-compound complex measured u | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9 | Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE). |
| AID1471805 | Reactivation of tabun inhibited human erythrocyte AChE assessed as reactivation rate constant using acetylthiocholine iodide as substrate preincubated up to 60 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1826694 | Reactivation of NIMP-inhibited recombinant His-TEV-tagged human AChE expressed in CHO-K1 cells assessed as reactivation constant, KD by measuring thiophenol levels by UV-vis absorption spectroscopy | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning. |
| AID552420 | Reactivation of DEP-mediated inactive human recombinant AChE at 10 uM after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID351912 | Reactivation of diisopropyl phosphorofluoridate-induced electric eel AChE inhibition at 0.1 mM by Ellman's method | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and evaluation of novel bis-pyridinium oximes as reactivators of DFP-inhibited acetylcholinesterase. |
| AID1471796 | Reactivation of cyclosarin inhibited human erythrocyte AChE assessed as residual activity at 10 to 1000 uM using acetylthiocholine iodide as substrate preincubated for 2 to 120 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID552419 | Reactivation of DEP-mediated inactive human recombinant AChE at 100 uM after 15 mins by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. |
| AID32123 | In vitro dissociation constant of rat brain Acetylcholinesterase (AChE)-reactivator complex was determined | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20 | Synthesis of a new reactivator of tabun-inhibited acetylcholinesterase. |
| AID1471798 | Reactivation of tabun inhibited human erythrocyte AChE assessed as residual activity at 10 to 1000 uM using acetylthiocholine iodide as substrate preincubated for 2 to 120 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Application of the Ugi Multicomponent Reaction in the Synthesis of Reactivators of Nerve Agent Inhibited Acetylcholinesterase. |
| AID1173382 | Reactivation of tabun-inhibited human acetylcholinesterase assessed as dissociation constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID1173381 | Reactivation of VX-inhibited human acetylcholinesterase assessed as dissociation constant | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID1173386 | Inhibition of human acetylcholinesterase by Ellman's method | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24 | New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase. |
| AID615410 | Reactivation of sarin-inhibited electric eel AChE activity after 40 mins by Ellman's method relative to control | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE). |
| AID1130947 | 1-Octanol-sodium phosphate buffer partition coefficient, log P of the compound at pH 7.4 at 25 degC by spectrophotometric analysis | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Antidotes or organophosphate poisoning. 2. Thiadiazole-5-carboxaldoximes. |
| AID260332 | Reactivation potency against inhibited AChE from rat brain homogenate at 1 mM | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase. |
| AID1076757 | Reactivation of cyclosarin OP-inactivated human plasma BChE assessed as reactivation rate constant using acetylthiocholine as substrate at 0.67 mM by spectrophotometric analysis | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification. |
| AID302661 | Binding affinity to tabun-inhibited AChE | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). |
| AID1076759 | Reactivation of sarin OP-inactivated human plasma BChE assessed as reactivation rate constant using acetylthiocholine as substrate at 0.67 mM by spectrophotometric analysis | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Imidazole aldoximes effective in assisting butyrylcholinesterase catalysis of organophosphate detoxification. |
| AID307192 | Reactivation of 1000 uM tabun-induced inhibition of AChE in rat brain at pH 7.6 after 10 mins | 2007 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11 | Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 104 (31.42) | 18.7374 |
| 1990's | 52 (15.71) | 18.2507 |
| 2000's | 91 (27.49) | 29.6817 |
| 2010's | 73 (22.05) | 24.3611 |
| 2020's | 11 (3.32) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (21.97) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 6 (1.80%) | 5.53% |
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 9 (2.70%) | 6.00% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 25 (7.51%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 293 (87.99%) | 84.16% |
| Other | 27 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Assessing The Role Of Intravenous Lipid Emulsion As A Life Saving Therapy In Pesticides Toxicity: A Randomized Controlled Trial In Poison Control Center Of Ain Shams University Hospitals [NCT05006638] | Phase 4 | 62 participants (Anticipated) | Interventional | 2022-12-31 | Recruiting | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||