Naslov
Derivati N-benzil-3-amidokinuklidina kao inhibitori butirilkolinesteraze
(N-BENZYL-3-AMIDOQUINUCLIDINE DERIVATIVES AS INHIBITORS OF BUTYRYLCHOLINESTERASE)

Autori
Odžak, Renata ; Tomić, Srđanka

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

Izvornik
XIX Hrvatski skup kemičara i kemijskih inženjera, Knjiga sažetaka / Škare, Danko - Zagreb : HKD i HDKIT, 2005

Skup
XIX Hrvatski skup kemičara i kemijskih inženjera

Mjesto i datum
Opatija, Hrvatska, 24.04.2005. - 27.04.2005

Vrsta sudjelovanja
Predavanje

Vrsta recenzije
Nije recenziran

Ključne riječi
butyrylcholinesterase; inhibition; 3-amidoquinuclidin; N-benzyl derivatives
(butirilkolinesteraza; inhibicija; 3-amidokinuklidin; N-benzil derivati)

Sažetak
Racemates as well as enantiomers of 3-amidoquinuclidine derivatives of acetic, pivalic, butyric and benzoic acid were prepared. Racemates and enantiomers of quaternary N-benzyl derivatives were synthesized as well by quaternization with benzyl bromide. Structures of all synthesized amides were established by spectroscopy (IR, MS, 1D and 2D NMR) and optical rotations measurements. Butyrylcholinesterase (BChE) was tested with a series of other enzymes as a possible biocatalyst in the hydrolysis of prepared racemic amides, but it was shown that hydrolysis did not occur. Taking into account this result and previously reported results on inhibitions of BChE by N-quaternary esters of quinuclidin-3-ol, N-benzyl amides were tested as possible inhibitors of BChE, as well. In experiments in which benzoylcholine was used as a substrate, it was shown that tested amides were inhibitors of BChE, the strongest of which was (S)-N-benzyl-3-benzamidoquinuclidinium bromide, (Ki=3.7 mikroM).

Izvorni jezik
Hrvatski

Znanstvena područja
Kemija

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