From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists

M J Tozer; E A Harper; S B Kalindjian; M J Pether; N P Shankley; G F Watt

doi:10.1016/s0960-894x(99)00272-3

From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1825-30. doi: 10.1016/s0960-894x(99)00272-3.

Authors

M J Tozer¹, E A Harper, S B Kalindjian, M J Pether, N P Shankley, G F Watt

Affiliation

¹ The James Black Foundation, London, UK. matthew.tozer@kcl.ac.uk

PMID: 10406649
DOI: 10.1016/s0960-894x(99)00272-3

Abstract

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.

MeSH terms

Animals
Drug Design*
Guinea Pigs
Histamine Antagonists / chemical synthesis*
Imidazoles / chemical synthesis*
Kinetics
Models, Chemical
Receptors, Histamine H3 / chemistry*
Sulfonamides / chemical synthesis*

Substances

Histamine Antagonists
Imidazoles
Receptors, Histamine H3
Sulfonamides