omega-(Imidazol-4-yl)alkane-1-sulfonamides: a new series of potent histamine H(3) receptor antagonists.
omega-(1H-Imidazol-4-yl)alkane-1-sulfonamides were prepared and found to be potent histamine H(3) receptor antagonists. High receptor affinity and a low difference in the data between the bioassays were achieved with 5-(1H-imidazol-4-yl)pentane-1-sulfonic acid 4-chlorobenzylamide (16). Good in vitro profiles were also obtained for 2-hydroxysulfonamide and vinylsulfonamide analogues. This complements and completes the existing set of imidazole-based sulfonamides and sulfamides.
Tozer
Matthew J
MJ
The James Black Foundation, 68 Half Moon Lane, Dulwich, SE24 9JE, London, UK. matt.tozer@medivir.com
Buck
Ildiko M
IM
Cooke
Tracey
T
Kalindjian
S Barret
SB
Pether
Michael J
MJ
Steel
Katherine I M
KI
D000818:Animals; D001593:Benzyl Compounds / Q000737:chemistry* / Q000494:pharmacology*; D001671:Biochemistry / Q000379:methods; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology*; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013329:Structure-Activity Relationship
C453039:5-(1H-imidazol-4-yl)pentane-1-sulfonic acid 4-chlorobenzylamide; D001593:Benzyl Compounds; D006633:Histamine Antagonists; D007093:Imidazoles; D018100:Receptors, Histamine H3