Introduction

Gupta, R.

doi:10.1016/b978-012088523-7/50002-8

Cited by 30 publications

(43 citation statements)

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“…The novel compounds also showed promising activity. Three of them (6,8,11) exceeded pralidoxime and HI-6 at a concentration 10 23 M. Moreover, two oximes (6, 11) reached or exceeded the activity of obidoxime at a concentration applicable in vivo. Finally, the oxime 11 surpassed all tested compounds in reactivation of paraoxon-inhibited AChE.…”

Section: Resultsmentioning

confidence: 99%

“…On the other hand, the recently developed reactivators (1-2) showed promising activity. In addition, there are two reactivators (8,11), in the synthesized compounds, which had some ability against GA-inhibited AChE, although poor. Compared to the known or recently developed compounds, the (8) exceeds all of these at both concentrations used.…”

Section: Resultsmentioning

confidence: 99%

“…(B) Preparation of bisquaternary salts -A solution of the monoquaternary salt (0.50 g, 1.5 mmol) and carbamoylpyridine (0.38 g, 3.0 mmol) in DMF (10 mL) was stirred at 80 -1008C. The reaction mixture was cooled to room temperature and portioned with acetone (50 mL); the crystalline crude product was collected by filtration, washed with acetone (3 £ 20 mL) and recrystallized from MeCN (6)(7)(8)(9)(10)(11). (6).…”

Section: Chemistrymentioning

confidence: 99%

“…The (E)-but-2-ene linker connecting the pyridinium rings is also in compound K075, which is slightly shorter than the saturated one, supplying the butane connecting chain in the molecule of K048. Six compounds (6)(7)(8)(9)(10)(11) were prepared using conventional synthetic procedures; five of them (7-11) have not been previously described in the literature (Figure 4). Firstly, the monoquaternary salts (12 -14) were synthesized using an excess of five equivalent of (E)-1,4-dibromobut-2-ene in acetone, where bi-products occur only in minor yields (Scheme 1).…”

Section: Introductionmentioning

confidence: 99%

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Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun- and paraoxon-inhibited acetylcholinesterase

Musílek

Holas

Kuča

et al. 2008

Journal of Enzyme Inhibition and Medicinal Chemistry

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Chemistrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun- and paraoxon-inhibited acetylcholinesterase

Musílek

Holas

Kuča

et al. 2008

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…[65] For example, methyl diphenyl diisocyanate (MDI), a key material in polyurethane synthesis, is produced by this route. Amine phosgenation involves carbamate intermediates, industrially interesting molecules per se (having end applications as foams, adhesives, [66] agrochemicals, [67] drugs, and prodrugs [68] ) and precursors to ureas [69] and to isocyanate, with a market of several million tons per year. [57] Because carbamates are potentially amenable to CO 2 chemistry, their industrial development as well as related isocyanate production could become a frontier of the industrial utilization of CO 2 (Scheme 3).…”

Section: Isocyanatesmentioning

confidence: 99%

Carbon Dioxide Recycling: Emerging Large‐Scale Technologies with Industrial Potential

et al. 2011

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This Review introduces this special issue of ChemSusChem dedicated to CO(2) recycling. Its aim is to offer an up-to-date overview of CO(2) chemical utilization (inorganic mineralization, organic carboxylation, reduction reactions, and biochemical conversion), as a continuation and extension of earlier books and reviews on this topic, but with a specific focus on large-volume routes and projects/pilot plants that are currently emerging at (pre-)industrial level. The Review also highlights how some of these routes will offer a valuable opportunity to introduce renewable energy into the existing energy and chemical infrastructure (i.e., "drop-in" renewable energy) by synthesis of chemicals from CO(2) that are easy to transport and store. CO(2) conversion therefore has the potential to become a key pillar of the sustainable and resource-efficient production of chemicals and energy from renewables.

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Reversible cholinesterase inhibitors as pretreatment for exposure to organophosphates. A review

Lorke

Petroianu

2018

J of Applied Toxicology

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Organophosphorus compounds (OPCs), inhibitors of acetylcholinesterase (AChE), are useful agents as pesticides, but also represent a serious health hazard. Standard therapy with atropine and established oxime-type enzyme reactivators (pralidoxime, obidoxime) is unsatisfactory. Better therapeutic results are obtained, when reversible AChE inhibitors are administered before OPC exposure. This review summarizes the history of such a pretreatment approach and sums up a set of experiments undertaken in search of compounds that are efficacious when given before a broad range of OPCs. The prophylactic efficacy of 10 known AChE inhibitors, either already used clinically for different indications (physostigmine, pyridostigmine, ranitidine, tiapride, tacrine, amiloride, metoclopramide, methylene blue) or developed for possible therapeutic use in the future (7-methoxytacrine, K-27) was compared, when administered before exposure to six chemically diverse OPCs in the same experimental setting: ethyl-paraoxon, methyl-paraoxon, diisopropylfluorophosphate, terbufos sulfone, azinphos-methyl and dicrotophos. The experimental oxime K-27 was the most efficacious compound, affording best protection, when administered before terbufos sulfone, azinphos-methyl and dicrotophos, second best before ethyl- and methyl-paraoxon exposure and third best before diisopropylfluorophosphate administration. This ranking was similar to that of physostigmine, which was superior to the Food and Drug Administration-approved pretreatment for soman with pyridostigmine. Tiapride, amiloride, metoclopramide, methylene blue and 7-methoxytacrine did not achieve protection. No correlation was observed between the IC of the reversible AChE inhibitors and their protective efficacy. These studies indicate that K-27 can be considered a very promising broad-spectrum prophylactic agent in case of imminent organophosphate exposure, which may be related to its AChE reactivating activity rather than its AChE inhibition.

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Introduction

Cited by 30 publications

References 0 publications

Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun- and paraoxon-inhibited acetylcholinesterase

Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun- and paraoxon-inhibited acetylcholinesterase

Carbon Dioxide Recycling: Emerging Large‐Scale Technologies with Industrial Potential

Reversible cholinesterase inhibitors as pretreatment for exposure to organophosphates. A review

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