Preparation, in vitro screening and molecular modelling of symmetrical 4-tert-butylpyridinium cholinesterase inhibitors—Analogues of SAD-128

…, J Roder, M Komloova, O Holas, M Hrabinova…

Index: Musilek, Kamil; Roder, Jan; Komloova, Marketa; Holas, Ondrej; Hrabinova, Martina; Pohanka, Miroslav; Dohnal, Vlastimil; Opletalova, Veronika; Kuca, Kamil; Jung, Young-Sik Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 1 p. 150 - 154

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Citation Number: 9

Abstract

Carbamate inhibitors (eg, pyridostimine bromide) are used as a pre-exposure treatment for the prevention of organophosphorus poisoning. They work by blocking acetylcholinesterase's (AChE) native function and thus protect AChE against irreversible inhibition by organophosphorus compounds. However, carbamate inhibitors are known for many undesirable side-effects related to the carbamylation of AChE. In this Letter, 19 ...