From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.
Histamine was converted to a selective histamine H3-receptor antagonist by capping the primary amine with 2-naphthalenesulfonyl chloride. Higher receptor affinity and lower variability in the data from the various bioassays were achieved with the 2-naphthalensulfonamides of histamine homologues.
The James Black Foundation, London, UK. matthew.tozer@kcl.ac.uk
M J
MJ
Tozer
E A
EA
Harper
S B
SB
Kalindjian
M J
MJ
Pether
N P
NP
Shankley
G F
GF
Watt
D000818:Animals; D015195:Drug Design; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000138:chemical synthesis*; D007093:Imidazoles / Q000138:chemical synthesis*; D007700:Kinetics; D008956:Models, Chemical; D018100:Receptors, Histamine H3 / Q000737:chemistry*; D013449:Sulfonamides / Q000138:chemical synthesis*
D006633:Histamine Antagonists; D007093:Imidazoles; D018100:Receptors, Histamine H3; D013449:Sulfonamides