Azines and diazines as potential histamine H3-receptor antagonists.
In search of structure-activity relationships among histamine H3-receptor antagonists the imidazole ring of known H3-receptor antagonists was replaced by different heteroaromatic ring systems. Thus, azines and diazines with ether (6-13) and carbamate (15-24) moieties as functional groups were synthesized. The obtained compounds did not show significant H3-receptor antagonist activity in vitro (rat brain cortex) or in vivo (mice brain). The new compounds were also screened for H1-receptor antagonist activity on the isolated guinea-pig ileum and for H2-receptor antagonist activity on the isolated spontaneously beating guinea-pig right atrium. The substances showed only weak antagonistic activity at both histamine receptors, H1 and H2.
Kieć-Kononowicz
K
K
Department of Chemical Technology of Drugs, Collegium Medicum, Jagiellonian University, Kraków, Poland.
Ligneau
X
X
Stark
H
H
Schwartz
J C
JC
Schunack
W
W
D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects; D006168:Guinea Pigs; D006633:Histamine Antagonists; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D051379:Mice; D009130:Muscle, Smooth / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D006633:Histamine Antagonists; D007093:Imidazoles; D011725:Pyridines