Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
We report the discovery of novel histamine H(3) receptor antagonists based on 4-[(1H-imidazol-4-yl)methyl]piperidine. The most potent compounds in the series (e.g., 7) result from the attachment of a substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker.
Vaccaro
Wayne D
WD
The Schering Plough Research Institute, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, USA.
Sher
Rosy
R
Berlin
Michael
M
Shih
Neng-Yang
NY
Aslanian
Robert
R
Schwerdt
John H
JH
McCormick
Kevin D
KD
Piwinski
John J
JJ
West
Robert E
RE
Anthes
John C
JC
Williams
Shirley M
SM
Wu
Ren-Long
RL
She
H Susan
HS
Rivelli
Maria A
MA
Mutter
Jennifer C
JC
Corboz
Michel R
MR
Hey
John A
JA
Favreau
Leonard
L
D065690:Cytochrome P-450 CYP2D6 Inhibitors; D004353:Drug Evaluation, Preclinical; D006633:Histamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013329:Structure-Activity Relationship
D065690:Cytochrome P-450 CYP2D6 Inhibitors; D006633:Histamine Antagonists; D007093:Imidazoles; D010880:Piperidines; D018100:Receptors, Histamine H3; C085755:4-(1H-imidazol-4-ylmethyl)piperidine