Bioorganic & Medicinal Chemistry Letters 1999-07-05

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

Index: Bioorg. Med. Chem. Lett. 9(13) , 1825-30, (1999)

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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.