4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists

M J Tozer; I M Buck; T Cooke; S B Kalindjian; I M McDonald; M J Pether; K I Steel

doi:10.1016/s0960-894x(99)00535-1

4-Chlorobenzyl sulfonamide and sulfamide derivatives of histamine homologues: the design of potent histamine H3 receptor antagonists

Bioorg Med Chem Lett. 1999 Nov 1;9(21):3103-8. doi: 10.1016/s0960-894x(99)00535-1.

Authors

M J Tozer¹, I M Buck, T Cooke, S B Kalindjian, I M McDonald, M J Pether, K I Steel

Affiliation

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

PMID: 10560733
DOI: 10.1016/s0960-894x(99)00535-1

Abstract

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.

MeSH terms

Animals
Drug Design
Guinea Pigs
Histamine / analogs & derivatives*
Histamine Antagonists / chemical synthesis*
Histamine Antagonists / pharmacology
Ileum / drug effects
Ileum / metabolism
Molecular Structure
Muscle Contraction / drug effects
Naphthalenes / chemical synthesis*
Naphthalenes / pharmacology
Receptors, Histamine H3 / drug effects*
Sulfonamides / chemical synthesis*
Sulfonamides / pharmacology

Substances

Histamine Antagonists
Naphthalenes
Receptors, Histamine H3
Sulfonamides
Histamine