4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists.
4-Chlorophenylmethanesulfonamide and (4-chlorobenzyl)sulfamide derivatives of histamine homologues were prepared and found to be potent and selective histamine H3 receptor antagonists. High receptor affinity and low differences in the data from the bioassays were achieved with the imidazol-4-ylbutyl analogues.
Tozer
M J
MJ
The James Black Foundation, London, UK. matthew.tozer@kcl.ac.uk
Buck
I M
IM
Cooke
T
T
Kalindjian
S B
SB
McDonald
I M
IM
Pether
M J
MJ
Steel
K I
KI
D000818:Animals; D015195:Drug Design; D006168:Guinea Pigs; D006632:Histamine / Q000031:analogs & derivatives*; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D009119:Muscle Contraction / Q000187:drug effects; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
D006633:Histamine Antagonists; D009281:Naphthalenes; D018100:Receptors, Histamine H3; D013449:Sulfonamides; D006632:Histamine