Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists.
A series of 2-(1,4'-bipiperidine-1'-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H(3) receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure-activity relationships for these new thiazolopyridine antagonists are discussed.
Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-1-1800, Kenilworth, NJ 07033, USA. ashwin.rao@spcorp.com
Ashwin U
AU
Rao
Anandan
A
Palani
Xiao
X
Chen
Ying
Y
Huang
Robert G
RG
Aslanian
Robert E
RE
West
Shirley M
SM
Williams
Ren-Long
RL
Wu
Joyce
J
Hwa
Christopher
C
Sondey
Jean
J
Lachowicz
D000818:Animals; D000882:Haplorhini; D006633:Histamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D051379:Mice; D008813:Mice, Inbred ICR; D008862:Microsomes, Liver / Q000378:metabolism; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D018100:Receptors, Histamine H3 / Q000737:chemistry* / Q000378:metabolism; D011994:Recombinant Proteins / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship; D015534:Trans-Activators / Q000378:metabolism; D000071230:Transcriptional Regulator ERG
C072312:ERG protein, human; D006633:Histamine Antagonists; D011725:Pyridines; D018100:Receptors, Histamine H3; D011994:Recombinant Proteins; D015534:Trans-Activators; D000071230:Transcriptional Regulator ERG