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Front Cover: Synthesis and Biological Evaluation of Nipecotic Acid and Guvacine Derived 1,3‐Disubstituted Allenes as Inhibitors of Murine GABA Transporter mGAT1 (ChemMedChem 12/2019)
Author(s) -
Schaarschmidt Maren,
Höfner Georg,
Wanner Klaus T.
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900336
Subject(s) - nipecotic acid , moiety , chemistry , gaba transporter , stereochemistry , front cover , transporter , biochemistry , receptor , cover (algebra) , mechanical engineering , neurotransmitter , gene , engineering
The Front Cover shows a new class of nipecotic acid derivatives as inhibitors (represented by the stop sign) of the Na + and Cl − dependent GABA transporter mGAT1 (represented by the bus). Compounds of the described class are defined by a unique terminally monosubstituted four‐carbon atom allenyl spacer connecting the nitrogen of the polar nipecotic acid subunit with a lipophilic aromatic residue. Data from MS Binding Assays and [ 3 H]GABA‐Uptake‐Assays revealed the influence of the linear and rigid allene moiety in the spacer on the binding affinity for mGAT1 and inhibitory potencies at mGAT1‐4 of this class of conformationally restricted GABA‐Uptake‐Inhibitors. Cover illustration by J. Pabel. More information can be found in the Full Paper by Klaus T. Wanner et al. on page 1135 in Issue 12, 2019 (DOI: 10.1002/cmdc.201900170).