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Preparation and in vitro screening of symmetrical bis-isoquinolinium cholinesterase inhibitors bearing various connecting linkage - Implications for early Myasthenia gravis treatment

Publication at Faculty of Pharmacy in Hradec Králové |
2011

Abstract

This paper describes preparation and in vitro evaluation of 20 newly prepared bis-isoquinolinium inhibitors of potential concern for Myasthenia gravis (MG). The newly prepared compounds were evaluated in vitro on human recombinant acetylcholinesterase (AChE) and human plasmatic butyrylcholinesterase (BChE).

Their inhibitory ability was expressed as IC50 and compared to chosen standards ambenonium dichloride, edrophonium chloride, BW284c51 and ethopropazine hydrochloride.