SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF 2-BENZYLOXY SUBSTITUTED ARYL KETONES AS 5-HT4 RECEPTOR ANTAGONISTS

Authors
CLARK RD JAHANGIR A LANGSTON JA WEINHARDT KK MILLER AB LEUNG E BONHAUS DW WONG EHF EGLEN RM
Citation
Rd. Clark et al., SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF 2-BENZYLOXY SUBSTITUTED ARYL KETONES AS 5-HT4 RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(20), 1994, pp. 2481-2484
Citations number
7
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
20
Year of publication
1994
Pages
2481 - 2484
Database
ISI
SICI code
0960-894X(1994)4:20<2481:SAPPEO>2.0.ZU;2-G
Abstract
Structural modification of the 2-methoxy group and at the 4-position o f the piperidine ring of the 5-HT4 partial agonist 1 led to analogues with increased affinity for the 5-HT4 receptor and loss of agonist act ivity. Similar modification of 2 resulted in 2-(3,5-dimethoxy)benzylox y derivatives (23,24,26-28) that were found to be 5-HT4 receptor antag onists with subnanomolar affinity.