Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists.
H(3)R inverse agonists based on an aminopropoxy-phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse model of recognition memory.
Célanire
Sylvain
S
UCB New Medicines, Chemin du Foriest, 1420 Braine-L'Alleud, Belgium.
Wijtmans
Maikel
M
Christophe
Bernard
B
Collart
Philippe
P
de Esch
Iwan
I
Dassesse
Donald
D
Delaunoy
Christel
C
Denonne
Frédéric
F
Durieu
Véronique
V
Gelens
Edith
E
Gillard
Michel
M
Lallemand
Bénédicte
B
Lamberty
Yves
Y
Lebon
Florence
F
Nicolas
Jean-Marie
JM
Quéré
Luc
L
Snip
Erwin
E
Vanbellinghen
Alain
A
Van Houtvin
Nathalie
N
Verbois
Valérie
V
Timmerman
Henk
H
Talaga
Patrice
P
Leurs
Rob
R
Provins
Laurent
L
D000818:Animals; D016466:CHO Cells; D018938:Caco-2 Cells; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D054314:Drug Inverse Agonism; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000737:chemistry; D051379:Mice; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017397:Prefrontal Cortex / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D018100:Receptors, Histamine H3 / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
D054828:Histamine H3 Antagonists; D007093:Imidazoles; D010080:Oxazoles; D018100:Receptors, Histamine H3; C029899:imidazole