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5‐HT 7 Receptor Antagonists with an Unprecedented Selectivity Profile
Author(s) -
Ates Ali,
Burssens Pierre,
Lorthioir Olivier,
Lo Brutto Patrick,
Dehon Gwenael,
Keyaerts Jean,
Coloretti Francis,
Lallemand Bénédicte,
Verbois Valérie,
Gillard Michel,
Vermeiren Céline
Publication year - 2018
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201800026
Subject(s) - selectivity , 5 ht receptor , receptor , 5 ht7 receptor , chemistry , serotonin , pharmacology , biology , biochemistry , catalysis
Selective leads : In this study, we generated a new series of serotonin 5‐HT 7 receptor antagonists. Their synthesis, structure–activity relationships, and selectivity profiles are reported. This series includes 5‐HT 7 antagonists with unprecedented high selectivity for the 5‐HT 7 receptor, setting the stage for lead optimization of drugs acting on a range of neurological targets.