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Synthesis of glucoconjugates with heterocyclic oximes (CROSBI ID 527400)

Prilog sa skupa u časopisu | sažetak izlaganja sa skupa | međunarodna recenzija

Odžak, Renata ; Oršulić, Mislav ; Tomić, Srđanka Synthesis of glucoconjugates with heterocyclic oximes // Toxicology / Szinicz, Ladislav (ur.). 2006. str. 54-x

Podaci o odgovornosti

Odžak, Renata ; Oršulić, Mislav ; Tomić, Srđanka

engleski

Synthesis of glucoconjugates with heterocyclic oximes

The heterocyclic parts of these conjugates were quinuclidinium, pyridinium or imidazolium oximes, basic structures of many compounds tested in vitro and in vivo as antidotes in poisoning by organophosphorus (OP) compounds such as pesticides and nerve warfare agents [1-3]. The OP compounds inhibit the enzyme acetylcholinesterase (AChE), essentially irreversibly. This causes accumulation of acetylcholine (ACh) which is responsible for many toxic effects. An oxime is considered to be an efficient antidote if it has a high reactivation rate constant and if it persists in blood circulation for a long enough period of time. Its toxicity should be low as well. The glucoconjugates on which we report in this work were designed as possible model compounds satisfying these requirements. It was previously found that attachment of a sugar moiety to the oxime derivatives increases the bioavailability of the antidote. Thus, we presume that the sugar moiety might be recognized by sites responsible for sugar transport trough the cell membrane leading to the increased permeability of membranes for the quaternary oximes. Furthermore, the previously reported glucoconjugates were less toxic than non-sugar conjugates, and some of them also displayed higher efficacy [4].

oximes; glucoconjugate

Toxicology, vol 233, issues 1-3, comprises 25 papers related to the main scope of the Conference and also 26 abstracts of the othe contributions

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Podaci o prilogu

54-x.

2006.

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objavljeno

Podaci o matičnoj publikaciji

Toxicology

Szinicz, Ladislav

München:

0300-483X

Podaci o skupu

10th International Medical Chemical Defence Conference (MCDC) 2006

poster

25.04.2006-27.04.2006

München, Njemačka

Povezanost rada

Kemija

Indeksiranost