| Literature DB >> 34034134 |
Charles J McElhinny1, Anita H Lewin1, Larry Brieaddy1, Scott Fix1, Gregory H Imler2, Jeffrey Deschamps2, S Wayne Mascarella1, Herbert H Seltzman1, P Anantha Reddy1, F Ivy Carroll1.
Abstract
Inconsistent results have been reported for the effects of the mitogen-activating extracellular kinase (MEK) inhibitor α-[amino(4-aminophenyl)thio]methylene-2-(trifluoromethyl)benzeneacetonitrile (SL 327) on ethanol-induced conditioned place preference (EtOH-CPP). Since such inconsistencies may be due to the configurational composition of administered SL 327, the interconvertibility of the geometric isomers of this class of compounds has been investigated. This study provides conditions for determination of configurational composition of this class of compounds by HPLC and by 1H NMR and reports details of configurational equilibria as a function of medium and time in solution along with solubility data for SL 327 in aqueous DMSO. The results suggest that the apparently inconsistent results reported for CPP-EtOH may be due to the administration of suspension vs. solutions, as well as to different configurational compositions of SL 327.Entities:
Keywords: E/Z configuration; Formulation; MEK inhibitor; SL 327; Solubility
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Year: 2021 PMID： 34034134 PMCID： PMC8217309 DOI： 10.1016/j.bioorg.2021.104955
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.307