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Pregled bibliografske jedinice broj: 648193

Preparation and in vitro screening of heterocyclic quaternary cholinesterase reactivators


Baumann, Krešimir; Primožič, Ines; Tomić-Pisarović, Srđanka
Preparation and in vitro screening of heterocyclic quaternary cholinesterase reactivators // Syntetic Life: Molecules, Cells and Tissues, Weizmann Institute of Science, Rehovot, Izrael, 13-16. 10. 2013.
Weizmann Institute of Science, Rehovot, Izrael, 2013. (poster, nije recenziran, neobjavljeni rad, znanstveni)


Naslov
Preparation and in vitro screening of heterocyclic quaternary cholinesterase reactivators

Autori
Baumann, Krešimir ; Primožič, Ines ; Tomić-Pisarović, Srđanka

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, neobjavljeni rad, znanstveni

Izvornik
Syntetic Life: Molecules, Cells and Tissues, Weizmann Institute of Science, Rehovot, Izrael, 13-16. 10. 2013. / - , 2013

Skup
Syntetic Life: Molecules, Cells and Tissues (Student Workshop)

Mjesto i datum
Weizmann Institute of Science, Rehovot, Izrael, 13-16.10.2013

Vrsta sudjelovanja
Poster

Vrsta recenzije
Nije recenziran

Ključne riječi
Antidotes; organophosphates; cholinesterases

Sažetak
Organophosphates (OP) and carbamates (CM) are extremely toxic cholinesterase inhibiting compounds used as pesticides, insecticides and nerve agents. In the past century, the development of OPs and CMs was greater than ever before, and will most likely continue due to discovery of new applications for these compounds. Chemical warfare agents are of outmost concern because of their possible use in wars and terrorist attacks. Since there is still no single, broad-spectrum compound suitable for the antidotal treatment of poisoning with all OP agents a series of novel aliphatic and aromatic quaternary salts of N-alkyl/aryl imidazole- and benzimidazole-2-aldoximes have been prepared as potential reactivators of inhibited cholinesterases. N-alkylations of commercially available heterocyclic azoles resulted in their N-alkyl/aryl derivatives. N-alkyl/aryl imidazoles and benzimidazoles were converted to the appropriate 2-carbaldehydes by using modified Ivesen-Lund method and then to 2-aldoximes. Reaction of the oximes with the alkyl/aryl halogenides resulted in a desired quaternary salts. Structures of prepared compounds were deduced from IR, one- and twodimensional NMR and MS spectra. Ellmans method4 and acetylthiocholine as substrate were used to test inhibitory properties of prepared compounds and their reactivation efficiency of Paraoxon™ inhibited HuBChE, as well as lyophilised EqBChE . Structural characteristics of an efficient oxime reactivator will be discussed.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekt / tema
119-1191344-3121 - Sinteze i enzimske transformacije biološki aktivnih spojeva (Srđanka Tomić-Pisarović, )

Ustanove
Prirodoslovno-matematički fakultet, Zagreb