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In Search of Potent 5‐HT6 Receptor Inverse Agonists
Author(s) -
Hostetler Greg,
Dunn Derek,
McKenna Beth Ann,
Kopec Karla,
Chatterjee Sankar
Publication year - 2014
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12279
Subject(s) - inverse agonist , enantiomer , chemistry , potency , stereochemistry , pharmacology , chirality (physics) , sulfonamide , selectivity , receptor , in vitro , agonist , biochemistry , medicine , nambu–jona lasinio model , chiral symmetry breaking , physics , quantum mechanics , quark , catalysis
A series of non‐sulfonamide/non‐sulfone derived potent 5‐HT 6 receptor inverse agonists has been disclosed. Representative compound 9 ( K i = 14 n m ) displayed selectivity against a set of family members as well as brain permeability 6 h post‐oral administration. In addition, the separated enantiomers of compound 9 displayed difference in activity indicating the influence of chirality on potency.