Synthesis and SAR of novel histamine H3 receptor antagonists.
The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H(3) receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored. Several compounds with high affinity and selectivity for the human and rat H(3) receptors are reported.
Jesudason
Cynthia D
CD
Lilly Research Laboratories, Eli Lilly & Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. jesudason_cynthia_d@lilly.com
Beavers
Lisa S
LS
Cramer
Jeffrey W
JW
Dill
Joelle
J
Finley
Don R
DR
Lindsley
Craig W
CW
Stevens
F Craig
FC
Gadski
Robert A
RA
Oldham
Samuel W
SW
Pickard
R Todd
RT
Siedem
Christopher S
CS
Sindelar
Dana K
DK
Singh
Ajay
A
Watson
Brian M
BM
Hipskind
Philip A
PA